Ligand source activities (1 row/activity)



Get vendors


Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
1185 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
1185 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3632 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
53386917 63174 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63174 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388960 63222 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800663 63222 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
11512905 137877 0 None 1778 2 Human 10.2 pIC50 = 10.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137877 0 None 1778 2 Human 10.2 pIC50 = 10.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
9961721 167903 0 None 60 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167903 0 None 60 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
53388958 63220 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800661 63220 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
18324807 63227 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63227 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
20691661 79188 0 None 138 2 Human 10.0 pIC50 = 10 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79188 0 None 138 2 Human 10.0 pIC50 = 10 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
10100930 63173 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63173 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386915 63171 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63171 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389117 63225 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800666 63225 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389115 63223 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800664 63223 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53387071 63175 4 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63175 4 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10371708 63176 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63176 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389118 63226 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800667 63226 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53386756 63228 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800669 63228 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44293301 187911 0 None - 1 Rat 9.5 pIC50 = 9.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50283 187911 0 None - 1 Rat 9.5 pIC50 = 9.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16221494 161391 0 None 8 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415659 161391 0 None 8 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
10348973 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
53386757 63229 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
CHEMBL1800670 63229 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
10100930 63173 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63173 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386917 63174 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63174 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
11421412 178154 11 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 178154 11 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11477988 90565 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90565 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
16155709 167899 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL435141 167899 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155709 167899 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL435141 167899 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 208791 8 None 1 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
101755083 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
16136245 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
4379 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
5585 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
CHEMBL415606 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
DB06699 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
101755083 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
16136245 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
4379 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
5585 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
CHEMBL415606 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
DB06699 1327 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
44293163 188105 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188105 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL407661 210918 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
11262242 188142 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 188142 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
16221267 141458 0 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL387499 141458 0 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
23656390 161122 0 None 4 2 Rat 9.2 pIC50 = 9.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 161122 0 None 4 2 Rat 9.2 pIC50 = 9.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
1184 3663 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3663 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3663 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
1184 3663 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3663 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3663 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL407661 210918 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 208791 8 None 1 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 208791 8 None 1 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL434380 211896 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H](C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)cc1 10.1021/jm060240a
44395623 124124 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL364167 124124 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL434380 211896 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H](C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)cc1 10.1021/jm060240a
16221104 85119 0 None 6 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227861 85119 0 None 6 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
87285768 169917 1 None 158 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169917 1 None 158 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
22129998 100792 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100792 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16156699 166002 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL427976 166002 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221266 165795 0 None 2 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL427438 165795 0 None 2 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
44395435 123282 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362371 123282 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16221495 85084 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227451 85084 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
16156699 166002 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL427976 166002 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
10348973 3249 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3249 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3249 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3249 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3249 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
9895596 63170 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63170 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
16221556 167775 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL434371 167775 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL429527 211778 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
155531714 175607 0 None 501 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175607 0 None 501 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL429527 211778 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221496 142203 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL389248 142203 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
16156573 168299 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438239 168299 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156573 168299 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438239 168299 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
10649568 14382 0 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL120432 14382 0 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL219061 207649 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL219061 207649 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
53387071 63175 4 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63175 4 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10371708 63176 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63176 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
10649568 14382 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Activity at human GnRH receptor by inositol phosphate functional assayActivity at human GnRH receptor by inositol phosphate functional assay
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm701249f
CHEMBL120432 14382 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Activity at human GnRH receptor by inositol phosphate functional assayActivity at human GnRH receptor by inositol phosphate functional assay
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm701249f
53386916 63172 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800154 63172 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10649568 14382 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Functional antagonism at the human GnRH receptor (PI turnover)Functional antagonism at the human GnRH receptor (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Functional antagonism at the human GnRH receptor (PI turnover)Functional antagonism at the human GnRH receptor (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44321052 204538 0 None - 1 Human 9.0 pIC50 = 9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86912 204538 0 None - 1 Human 9.0 pIC50 = 9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
16155593 157879 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409044 157879 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155593 157879 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409044 157879 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409043 210986 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409043 210986 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16221433 141619 0 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL388369 141619 0 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16221211 168685 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL441211 168685 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
44432651 86262 0 None 21 2 Rat 8.9 pIC50 = 8.9 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 86262 0 None 21 2 Rat 8.9 pIC50 = 8.9 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
53386915 63171 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63171 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44395650 168744 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL441676 168744 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL2105773 210984 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL409018 210984 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16155157 95988 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL262180 95988 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398152 159656 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 42 17 20 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL410967 159656 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 42 17 20 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16155157 95988 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL262180 95988 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL2105773 210984 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL409018 210984 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
18324807 63227 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63227 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL2105773 210984 7 None 1 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL409018 210984 7 None 1 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
44321964 95959 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL261979 95959 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
16156328 96191 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL263691 96191 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398047 96452 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL265879 96452 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16156328 96191 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL263691 96191 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376654 210496 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376654 210496 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398065 155160 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1671 41 17 18 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL405273 155160 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1671 41 17 18 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
11250647 1510 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 1510 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 1510 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 1510 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 1510 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44449120 94776 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94776 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL262747 208791 8 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44380487 167007 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL430069 167007 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
23656390 161122 0 None -4 2 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 161122 0 None -4 2 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL219562 207662 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)CNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL219562 207662 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)CNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
44398064 166446 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1647 40 17 20 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL428825 166446 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1647 40 17 20 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
145957953 161569 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 633 9 1 9 4.3 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4161566 161569 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 633 9 1 9 4.3 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
44398063 161248 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414347 161248 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
58239302 161429 0 None 616 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 161429 0 None 616 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44395462 167649 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL433594 167649 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16155358 137595 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376728 137595 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398043 161136 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1603 37 17 18 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL413450 161136 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1603 37 17 18 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16155358 137595 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376728 137595 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
101755083 1327 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
16136245 1327 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
4379 1327 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
5585 1327 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
CHEMBL415606 1327 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
DB06699 1327 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
16156341 161170 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL413688 161170 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156341 161170 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL413688 161170 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155098 160106 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411337 160106 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155098 160106 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411337 160106 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221267 141458 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL387499 141458 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
16221266 165795 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL427438 165795 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
44398150 96240 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 40 17 18 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL264090 96240 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 40 17 18 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398066 96685 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1701 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNC(C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL267873 96685 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1701 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNC(C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398045 161405 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1715 40 19 20 -1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)[C@H]1CC(=O)NC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415820 161405 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1715 40 19 20 -1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)[C@H]1CC(=O)NC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44293111 100735 0 None -5 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 100735 0 None -5 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44398151 161389 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1689 43 17 20 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415595 161389 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1689 43 17 20 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398046 160767 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N(C)[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL412500 160767 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N(C)[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
1185 3632 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3632 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3632 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3632 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
44320921 106672 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316362 106672 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44398135 96343 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 41 16 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN(C)CCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL265020 96343 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 41 16 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN(C)CCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398001 168378 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL438905 168378 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
10004181 100604 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL294910 100604 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292974 100912 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297238 100912 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44460342 167348 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL431402 167348 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
16656823 128128 0 None - 1 Human 8.0 pIC50 = 8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 468 5 2 6 4.3 CC(C)(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
CHEMBL3668011 128128 0 None - 1 Human 8.0 pIC50 = 8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 468 5 2 6 4.3 CC(C)(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
11191675 63037 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63037 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63037 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
1185 3632 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3632 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3632 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3632 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
44380317 167913 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL435262 167913 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44359191 12085 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 12085 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 12085 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44398121 96172 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
77232195 96172 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL263507 96172 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16145131 158921 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361540 158921 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL410165 158921 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361888 141232 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL386105 141232 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2369138 207842 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44380222 57276 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166778 57276 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293010 173665 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 472 7 2 8 5.0 O=[N+]([O-])c1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45490 173665 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 472 7 2 8 5.0 O=[N+]([O-])c1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
1179 945 31 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 945 31 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 945 31 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
44434414 88084 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
CHEMBL235179 88084 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
44293594 101083 0 None -10 2 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 101083 0 None -10 2 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293349 183532 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48273 183532 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
145993478 166755 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
CHEMBL4294163 166755 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
44577102 177941 0 None - 1 Human 5.0 pIC50 = 5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 303 5 1 4 4.1 CCSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1021/jm701249f
CHEMBL466735 177941 0 None - 1 Human 5.0 pIC50 = 5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 303 5 1 4 4.1 CCSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1021/jm701249f
118098039 128122 0 None - 1 Human 7.0 pIC50 = 7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 461 4 1 6 3.5 Cc1cccc(N(C)S(=O)(=O)c2ccc(Cl)c(-n3c(=O)[nH]c4sccc4c3=O)c2)c1 nan
CHEMBL3668005 128122 0 None - 1 Human 7.0 pIC50 = 7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 461 4 1 6 3.5 Cc1cccc(N(C)S(=O)(=O)c2ccc(Cl)c(-n3c(=O)[nH]c4sccc4c3=O)c2)c1 nan
44380681 58451 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168726 58451 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44341198 112546 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL331144 112546 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
145959547 161721 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1ccccc1C(N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4164102 161721 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1ccccc1C(N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
44359191 12085 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 12085 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 12085 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11467552 172132 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 172132 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44561397 189222 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189222 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341197 108535 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL321258 108535 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
44321394 106443 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
CHEMBL314860 106443 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
44395677 66390 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185738 66390 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380538 58761 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169620 58761 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380318 119860 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353308 119860 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44293151 100692 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 100692 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44432638 86343 0 None 10 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 86343 0 None 10 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
44451397 95445 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259220 95445 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44444665 93754 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 93754 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44432638 86343 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 86343 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
10208964 66334 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185438 66334 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44444676 154387 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 154387 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444628 93870 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 93870 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44340929 112990 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL332049 112990 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293591 101112 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101112 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44572286 180209 0 None -6 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180209 0 None -6 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11237922 65174 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1021/jm701249f
CHEMBL183066 65174 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1021/jm701249f
44293194 185843 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48763 185843 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
44292919 100663 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100663 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
25193798 169620 0 None 2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 169620 0 None 2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44293802 101549 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 101549 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293273 161531 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL416102 161531 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293164 167257 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL430763 167257 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44321496 105470 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL312995 105470 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
145980339 166023 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4280124 166023 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
44359333 11510 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 11510 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 11510 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44361524 168018 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1623 40 15 17 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435925 168018 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1623 40 15 17 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44444632 93871 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250569 93871 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
9895596 63170 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63170 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
16221557 165452 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL425486 165452 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
44573276 186823 0 None 4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 186823 0 None 4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
44321100 106596 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315909 106596 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380394 119430 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL349638 119430 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44398117 161404 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1649 43 19 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415813 161404 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1649 43 19 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44358957 12023 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184158 12023 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336039 12023 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293070 165531 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 165531 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914248 187138 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 187138 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293335 172048 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172048 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293195 184700 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL48592 184700 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44293165 101210 0 None -7 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 101210 0 None -7 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44380212 57298 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166843 57298 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44434437 150429 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395826 150429 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44359254 11512 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL1180716 11512 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL139292 11512 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
44434412 161216 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1565 39 4 26 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL414045 161216 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1565 39 4 26 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44572236 171323 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171323 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11496945 175891 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175891 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
24825725 192017 0 None 7 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 192017 0 None 7 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44321510 106642 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316159 106642 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
9983568 98512 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98512 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44215053 185028 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 185028 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44359285 11507 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 11507 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 11507 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44572287 180211 0 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 180211 0 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44292990 100715 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL295731 100715 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293348 100013 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100013 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293487 101150 0 None -2 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 101150 0 None -2 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936150 188140 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50500 188140 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145952400 162173 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2ccccc2F)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4171296 162173 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2ccccc2F)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
145950534 162243 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2cccc(F)c2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172405 162243 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2cccc(F)c2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44293605 100691 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295591 100691 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
10209293 100719 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295791 100719 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
24825725 192017 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192017 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
12283 2282 12 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
16656889 2282 12 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
CHEMBL3668014 2282 12 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
16656891 128131 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 522 9 2 8 3.5 COCCOc1ccc(F)c(F)c1COc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668015 128131 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 522 9 2 8 3.5 COCCOc1ccc(F)c(F)c1COc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
10438167 100699 0 None 15 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 100699 0 None 15 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44293803 188285 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 188285 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
20691661 79188 0 None 138 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79188 0 None 138 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
145953549 161855 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 2 9 4.0 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4166067 161855 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 2 9 4.0 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44293054 101012 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 101012 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292919 100663 0 None 2 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100663 0 None 2 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
15602808 8010 0 None -5 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8010 0 None -5 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44561368 176230 0 None -42 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176230 0 None -42 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44434435 88120 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1575 36 6 25 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235361 88120 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1575 36 6 25 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44572286 180209 0 None 6 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180209 0 None 6 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293222 175377 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 175377 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 175377 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
9958318 89782 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89782 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44293348 100013 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100013 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44432653 86263 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 86263 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44380146 119758 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352565 119758 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44293062 186115 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)cc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48853 186115 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)cc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44577104 178159 0 None -7 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178159 0 None -7 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
145973813 162461 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1cccc(C(N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4175816 162461 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1cccc(C(N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44293053 101009 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 101009 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293803 188285 0 None -1 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 188285 0 None -1 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293651 162552 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417726 162552 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432656 158600 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL409825 158600 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444641 154418 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 154418 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143420 162346 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4173938 162346 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44359458 12026 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 12026 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 12026 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
145955260 161972 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccc(F)cc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167957 161972 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccc(F)cc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
16656887 128129 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 504 6 2 7 4.8 COc1ccc(F)cc1C(C)(C)Sc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668012 128129 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 504 6 2 7 4.8 COc1ccc(F)cc1C(C)(C)Sc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44380551 58435 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168649 58435 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
145955571 162097 0 None -131 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 162097 0 None -131 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
44293555 100727 0 None -141 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295897 100727 0 None -141 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44444649 154454 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 154454 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44398149 160735 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1621 40 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL412212 160735 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1621 40 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44293041 100857 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL296819 100857 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
44292833 101057 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 480 7 2 7 5.5 Cc1cc(CC#N)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL298278 101057 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 480 7 2 7 5.5 Cc1cc(CC#N)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292733 176199 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 548 7 4 5 6.8 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL46060 176199 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 548 7 4 5 6.8 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
10348973 3249 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3249 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3249 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3249 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3249 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
44577104 178159 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178159 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44293249 184851 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL48616 184851 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
10077523 122186 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL360429 122186 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395463 126241 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL365366 126241 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44215055 100807 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 100807 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293249 184851 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 184851 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
21899433 154152 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 154152 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44341081 167490 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL432450 167490 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
16656822 128127 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 455 4 2 6 3.4 CN(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
CHEMBL3668010 128127 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 455 4 2 6 3.4 CN(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
44359333 11510 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 11510 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 11510 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293347 162549 0 None 4 2 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 162549 0 None 4 2 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293592 162328 0 None -4 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162328 0 None -4 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44434434 147529 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1531 33 6 24 8.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL393486 147529 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1531 33 6 24 8.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434392 168421 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1389 27 4 22 9.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL439200 168421 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1389 27 4 22 9.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44444652 94053 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 94053 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44293111 100735 0 None -5 2 Rat 5.7 pIC50 = 5.7 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 100735 0 None -5 2 Rat 5.7 pIC50 = 5.7 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44444642 93921 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 93921 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
58022100 128120 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2ccsc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
CHEMBL3668003 128120 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2ccsc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
138978203 166136 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
CHEMBL4282476 166136 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
145984647 165852 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4277116 165852 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978207 166589 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
CHEMBL4290761 166589 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
16657781 128123 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 517 4 2 7 3.2 O=C(O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
CHEMBL3668006 128123 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 517 4 2 7 3.2 O=C(O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
44380798 58999 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170606 58999 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380537 96100 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL263004 96100 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL2371821 208374 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN[C@H](C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL438629 212025 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438629 212025 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL2371822 208375 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None C#C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16156049 96322 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264781 96322 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16156049 96322 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264781 96322 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
102090748 161246 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
16138575 161246 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL414344 161246 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44395491 123319 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362544 123319 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10053165 183407 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL48192 183407 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44398044 154680 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 38 17 18 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL402683 154680 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 38 17 18 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16221433 141619 0 None -1 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL388369 141619 0 None -1 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16221494 161391 0 None -8 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415659 161391 0 None -8 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
9873212 57257 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166649 57257 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
10008768 58411 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168563 58411 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL268450 209000 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268450 209000 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
11365653 173608 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 173608 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44448991 154790 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154790 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154790 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44320895 163699 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL421160 163699 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
44380626 58404 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168539 58404 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
16155654 165514 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL425813 165514 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155654 165514 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL425813 165514 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398178 161268 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 43 18 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414507 161268 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 43 18 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44361795 167922 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435322 167922 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL269711 209046 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
21036877 173068 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 173068 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11167850 2691 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 2691 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 2691 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 2691 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
44321101 96387 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265288 96387 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
9960399 50256 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL157412 50256 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44398040 168235 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1681 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL437672 168235 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1681 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL264779 208875 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268813 209010 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264779 208875 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268813 209010 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44293195 184700 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL48592 184700 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
15602804 7983 0 None 70 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7983 0 None 70 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44340928 9637 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113432 9637 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
16656888 128130 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 488 5 2 7 3.3 CC(C)(c1ccccc1)S(=O)(=O)c1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668013 128130 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 488 5 2 7 3.3 CC(C)(c1ccccc1)S(=O)(=O)c1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44293058 101510 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 483 6 2 6 6.4 CC(C)(C)c1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1 10.1016/s0960-894x(00)00318-8
CHEMBL301552 101510 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 483 6 2 6 6.4 CC(C)(C)c1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1 10.1016/s0960-894x(00)00318-8
24825725 192017 0 None -7 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192017 0 None -7 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44293484 96255 0 None -64 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL264193 96255 0 None -64 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
44214069 100835 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL296644 100835 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
16221614 136012 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
CHEMBL373725 136012 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
44432646 146689 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 146689 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444639 154416 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 154416 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
44321498 204572 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87099 204572 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44359471 12077 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 12077 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 12077 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44444672 168825 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 168825 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44293074 187190 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 187190 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44561108 185838 0 None 4 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 185838 0 None 4 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44444670 94030 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 94030 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444673 93834 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 93834 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
145954439 162094 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 622 9 1 9 4.0 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169864 162094 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 622 9 1 9 4.0 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44341046 9966 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL115365 9966 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44359301 11516 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180754 11516 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141221 11516 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293488 101071 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 101071 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293335 172048 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172048 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44432657 148923 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394613 148923 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44398396 161362 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1737 44 17 20 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCN(c1ccccn1)c1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415328 161362 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1737 44 17 20 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCN(c1ccccn1)c1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
9845762 186234 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccs3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48938 186234 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccs3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44444675 154172 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 154172 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44321497 97629 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL273390 97629 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44293076 101338 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300268 101338 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293222 175377 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 175377 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 175377 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293126 161754 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 467 6 2 7 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL416459 161754 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 467 6 2 7 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292747 187347 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 494 7 4 5 5.8 Cc1cccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49695 187347 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 494 7 4 5 5.8 Cc1cccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44587394 171896 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL448253 171896 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44573110 186601 0 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 186601 0 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
71449058 83971 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 83971 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 83971 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
25193700 172701 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 172701 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44293163 188105 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188105 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44444668 153733 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 153733 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44434389 168327 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 838 21 2 14 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL438504 168327 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 838 21 2 14 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44292661 101306 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL300048 101306 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44561369 189864 0 None 15 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189864 0 None 15 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341082 9670 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113574 9670 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
11620431 178779 0 None -21 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178779 0 None -21 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11496945 175891 0 None -17 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175891 0 None -17 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10258659 12078 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 12078 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 12078 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293208 170567 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL445848 170567 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292940 100781 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296244 100781 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293511 100803 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 100803 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293377 101420 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 101420 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293236 174297 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL45639 174297 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
54584354 60911 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766108 60911 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
44293112 186702 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49293 186702 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16221434 96726 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL268297 96726 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
44593424 175549 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175549 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44593424 175549 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175549 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341199 112547 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL331145 112547 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44398119 96797 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1646 41 18 19 -0.4 CNC(=O)C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL268829 96797 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1646 41 18 19 -0.4 CNC(=O)C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44359252 11511 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180715 11511 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139291 11511 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432628 87313 0 None 13 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 87313 0 None 13 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
44448991 154790 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154790 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154790 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44293223 173719 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45501 173719 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44434387 152231 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 750 15 2 12 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL397360 152231 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 750 15 2 12 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44587393 172055 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449468 172055 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44341164 9458 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112378 9458 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
44432651 86262 0 None -21 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 86262 0 None -21 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
15602805 8008 0 None -11 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8008 0 None -11 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44293376 101192 0 None 1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 101192 0 None 1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293594 101083 0 None 10 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 101083 0 None 10 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293131 188242 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50663 188242 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293650 161767 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL416470 161767 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432641 166931 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL429976 166931 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
44292878 174388 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 441 6 2 6 5.4 Cc1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45661 174388 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 441 6 2 6 5.4 Cc1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
25156400 188262 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL506877 188262 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11214860 84333 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84333 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
44380483 58751 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169569 58751 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
44292835 180663 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 526 10 2 7 6.2 CCN(CC)Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL47618 180663 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 526 10 2 7 6.2 CCN(CC)Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
1185 3632 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3632 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3632 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3632 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
18914272 169103 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 169103 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44432640 154422 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 154422 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
16656819 128125 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 530 4 2 7 2.9 CNC(=O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
CHEMBL3668008 128125 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 530 4 2 7 2.9 CNC(=O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
145949496 162296 0 None -165 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 162296 0 None -165 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
11496610 4000 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4000 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4000 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
11496610 4000 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4000 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4000 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44432653 86263 0 None -1 2 Rat 7.6 pIC50 = 7.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 86263 0 None -1 2 Rat 7.6 pIC50 = 7.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444647 154450 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 154450 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
44432640 154422 0 None -1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 154422 0 None -1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
25194090 188331 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL507973 188331 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44292983 100753 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL296084 100753 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44444635 154154 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 154154 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
16656821 128126 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 474 6 2 7 3.9 COc1cccc(F)c1C(C)Oc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668009 128126 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 474 6 2 7 3.9 COc1cccc(F)c1C(C)Oc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
16656892 128133 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 491 6 2 7 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1CN(C)c1c(F)cccc1F nan
CHEMBL3668017 128133 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 491 6 2 7 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1CN(C)c1c(F)cccc1F nan
44293305 100978 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 100978 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
10032223 12082 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 12082 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 12082 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
16146022 169541 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL444381 169541 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
9918188 154171 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 154171 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44444626 154332 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 154332 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
16221212 165767 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL427269 165767 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
145954419 162067 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 9 1 9 4.4 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4169486 162067 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 9 1 9 4.4 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
16156517 160168 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411381 160168 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL219532 207661 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156517 160168 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411381 160168 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL219532 207661 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
54582417 60909 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
CHEMBL1766106 60909 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
25156943 187843 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL502341 187843 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
16221211 168685 0 None -2 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL441211 168685 0 None -2 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL2370890 208190 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44449681 95586 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL259906 95586 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
9872676 77811 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77811 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
9893269 65949 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL184819 65949 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16155218 166258 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL428484 166258 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155218 166258 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL428484 166258 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398182 161385 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1635 42 19 19 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415549 161385 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1635 42 19 19 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
1188 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
16131215 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
35 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1252 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB00106 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1251 206909 21 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44398179 161247 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1674 44 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414346 161247 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1674 44 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44321963 105448 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
CHEMBL312864 105448 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
44380536 119872 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353395 119872 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44293378 101410 0 None -37 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300792 101410 0 None -37 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
10985312 78321 0 None 91 2 Human 6.5 pIC50 = 6.5 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78321 0 None 91 2 Human 6.5 pIC50 = 6.5 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44434390 151099 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 882 24 2 15 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL396385 151099 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 882 24 2 15 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44434438 145650 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392008 145650 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44321458 105472 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313004 105472 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380192 57131 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57131 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44434402 146206 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1433 30 4 23 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392433 146206 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1433 30 4 23 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
145958075 161750 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 10 1 10 3.7 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4164522 161750 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 10 1 10 3.7 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
10258643 100900 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297151 100900 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44395502 165334 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL424991 165334 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44432647 86299 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231954 86299 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11496610 4000 11 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4000 11 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4000 11 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
44292838 101034 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 101034 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44359264 11508 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 11508 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 11508 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44292974 100912 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297238 100912 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44380796 58876 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170159 58876 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44293804 101316 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Compound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsCompound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300095 101316 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Compound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsCompound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44214098 100811 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296483 100811 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
15602807 8121 0 None -8 2 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8121 0 None -8 2 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44561141 192887 0 None 37 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 192887 0 None 37 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44577069 178129 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccccc3OC)ccc2n1Cc1ccccc1 10.1021/jm701249f
CHEMBL468348 178129 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccccc3OC)ccc2n1Cc1ccccc1 10.1021/jm701249f
44432628 87313 0 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 87313 0 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
10649568 14382 0 None 4 2 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None 4 2 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44293130 181300 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47791 181300 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44434411 146208 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392434 146208 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44444678 154388 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 154388 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
44293085 97850 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3Cl)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL274952 97850 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3Cl)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
11496610 4000 11 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4000 11 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4000 11 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44359456 12083 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184286 12083 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342908 12083 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293617 188080 0 None -23 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 188080 0 None -23 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293134 186808 0 None 1 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186808 0 None 1 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44434388 89360 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 794 18 2 13 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL237729 89360 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 794 18 2 13 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44341186 9934 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL115192 9934 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
22129998 100792 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100792 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
11477970 89055 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89055 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44293377 101420 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 101420 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293802 101549 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 101549 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145957253 161633 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 737 14 2 10 4.9 COc1ccc(F)cc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
CHEMBL4162619 161633 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 737 14 2 10 4.9 COc1ccc(F)cc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
44292888 174196 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45614 174196 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292918 170839 0 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170839 0 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44215908 93781 0 None -4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 93781 0 None -4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
16221329 136011 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
CHEMBL373724 136011 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
44449120 94776 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94776 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
16221613 166430 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL428795 166430 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
15602808 8010 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8010 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44321146 105911 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313946 105911 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44593425 176181 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176181 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44593425 176181 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 176181 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
44321410 106512 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315325 106512 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321393 204537 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86911 204537 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
11226531 99046 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99046 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
10985312 78321 0 None 91 2 Human 8.4 pIC50 = 8.4 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78321 0 None 91 2 Human 8.4 pIC50 = 8.4 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
16156639 137471 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376466 137471 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16156639 137471 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376466 137471 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
1190 867 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
25074887 867 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
583 867 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1200490 867 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB00050 867 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
44398180 155474 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1696 42 18 19 2.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL406225 155474 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1696 42 18 19 2.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16147767 96897 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL269516 96897 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16221104 85119 0 None -6 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227861 85119 0 None -6 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44380625 58403 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168538 58403 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
9894997 119795 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352806 119795 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
16155412 160606 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL411749 160606 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155412 160606 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL411749 160606 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16221150 161374 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415432 161374 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
9938925 57272 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166763 57272 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380478 58432 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168637 58432 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
145955571 162097 0 None 131 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 162097 0 None 131 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
11331001 188425 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 188425 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
16156572 166549 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL429016 166549 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
22130002 176118 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 505 6 2 6 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL45990 176118 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 505 6 2 6 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292829 176295 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 471 7 2 7 5.4 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL46157 176295 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 471 7 2 7 5.4 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
44292621 176430 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46288 176430 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
9959121 187765 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50120 187765 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
21254089 181065 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 181065 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293376 101192 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 101192 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44292984 176817 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c(C)c1 10.1016/s0960-894x(00)00318-8
CHEMBL46383 176817 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c(C)c1 10.1016/s0960-894x(00)00318-8
11583756 189052 0 None 31 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 189052 0 None 31 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
21254068 101305 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 101305 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293488 101071 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 101071 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293592 162328 0 None 4 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162328 0 None 4 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293148 186893 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49412 186893 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
11532637 7618 0 None 4 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7618 0 None 4 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44561397 189222 0 None -4 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189222 0 None -4 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44292608 177804 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 427 6 2 6 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46550 177804 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 427 6 2 6 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44577103 178158 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 530 10 4 9 4.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(O)NC)c21 10.1021/jm701249f
CHEMBL468564 178158 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 530 10 4 9 4.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(O)NC)c21 10.1021/jm701249f
44432645 86760 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232752 86760 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
16048665 128132 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1COc1c(OC)ccc(F)c1F nan
CHEMBL3668016 128132 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1COc1c(OC)ccc(F)c1F nan
18914263 96440 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 96440 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
11532637 7618 0 None -4 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7618 0 None -4 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44380192 57131 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57131 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
11634198 186773 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 186773 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44380624 58811 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169873 58811 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293274 100773 0 None -9 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 100773 0 None -9 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
11604354 186931 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 186931 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
44572235 188907 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188907 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44359458 12026 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 12026 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 12026 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432654 159236 0 None -6 2 Rat 7.4 pIC50 = 7.4 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 159236 0 None -6 2 Rat 7.4 pIC50 = 7.4 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451342 96005 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262334 96005 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
15602804 7983 0 None -70 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7983 0 None -70 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44444630 154273 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 154273 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44293101 186525 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 513 8 2 8 5.5 CC(=O)OCc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49162 186525 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 513 8 2 8 5.5 CC(=O)OCc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
145951481 162393 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 10 1 10 3.6 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4174753 162393 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 10 1 10 3.6 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
25193797 189063 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 189063 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44593415 188780 0 None 20 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188780 0 None 20 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44444617 93698 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 93698 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44380319 58427 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168615 58427 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44451319 95715 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260647 95715 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451396 156120 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406958 156120 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
25113693 161353 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL415279 161353 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44432639 86521 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL232356 86521 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
10209293 100719 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295791 100719 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44434431 88069 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 909 24 3 15 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235132 88069 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 909 24 3 15 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
11331001 188425 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509075 188425 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432642 153048 0 None 1 2 Rat 7.3 pIC50 = 7.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 153048 0 None 1 2 Rat 7.3 pIC50 = 7.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293591 101112 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101112 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44432635 86342 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 86342 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
44341056 114023 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL333614 114023 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
44398120 155739 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 41 17 19 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(=O)N(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL406535 155739 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 41 17 19 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(=O)N(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44561369 189864 0 None -15 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189864 0 None -15 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44432646 146689 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 146689 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44358962 12022 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184155 12022 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL335764 12022 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44395583 123814 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL363663 123814 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL268875 209016 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
15602805 8008 0 None 11 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8008 0 None 11 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44295755 192509 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 192509 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 192509 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380513 119673 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL351836 119673 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380147 119759 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352566 119759 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
1184 3663 31 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 3663 31 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 3663 31 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
16156572 166549 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL429016 166549 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398395 96519 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1751 45 17 20 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CN(Cc1ccccn1)Cc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL266444 96519 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1751 45 17 20 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CN(Cc1ccccn1)Cc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44448991 154790 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154790 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154790 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
16146554 160900 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
CHEMBL412749 160900 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
10051739 84994 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 84994 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44398181 155129 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1710 43 18 19 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL404973 155129 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1710 43 18 19 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16147453 96657 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL267622 96657 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
9808288 110980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL327704 110980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11421518 164733 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164733 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
9808288 110980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL327704 110980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
44361796 82965 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL219461 82965 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44395533 66450 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185986 66450 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380148 119792 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352782 119792 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
9985901 109951 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL324654 109951 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
71449058 83971 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 83971 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 83971 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
145991962 166268 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4285058 166268 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
44292988 181849 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 181849 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293411 188172 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50552 188172 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44359287 11515 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 11515 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 11515 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293163 188105 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188105 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44398086 96575 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL266893 96575 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44451379 168403 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL439076 168403 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44359471 12077 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 12077 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 12077 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44434428 146209 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 865 21 3 14 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392435 146209 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 865 21 3 14 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44292606 101061 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 445 6 2 6 5.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL298300 101061 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 445 6 2 6 5.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292862 181055 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 477 6 2 6 6.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL47758 181055 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 477 6 2 6 6.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293486 186824 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 186824 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44572287 180211 0 None -9 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 180211 0 None -9 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293366 161650 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 161650 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293250 101250 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 101250 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44432636 86943 0 None -8 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 86943 0 None -8 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44460343 203624 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL79639 203624 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293301 187911 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50283 187911 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44432643 146222 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 146222 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293274 100773 0 None 9 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 100773 0 None 9 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
22100905 183674 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 183674 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44593425 176181 0 None -12 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176181 0 None -12 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44293250 101250 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 101250 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
58239302 161429 0 None -616 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 161429 0 None -616 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11583756 189052 0 None -31 2 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 189052 0 None -31 2 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44359193 11518 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180764 11518 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141750 11518 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293323 100733 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295911 100733 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
22129993 178140 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 558 7 4 5 6.2 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL46844 178140 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 558 7 4 5 6.2 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
44292745 187321 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1ccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL49667 187321 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1ccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
16144515 155574 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL406337 155574 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
11249548 98620 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98620 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
16221328 85159 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL228197 85159 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
145949496 162296 0 None 165 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 162296 0 None 165 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
44361802 168272 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL438018 168272 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44340906 9465 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112400 9465 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
44321291 204544 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86950 204544 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
10032223 12082 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 12082 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 12082 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432652 96680 0 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 96680 0 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44380514 119694 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352051 119694 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL262747 208791 8 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44321292 204553 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87000 204553 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380797 58965 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170499 58965 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL2105773 210984 7 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL409018 210984 7 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16221151 143052 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL389945 143052 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
15602806 8197 0 None 7 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8197 0 None 7 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44432648 149682 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 149682 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44292728 100754 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 487 8 2 8 5.1 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1OC 10.1016/s0960-894x(00)00318-8
CHEMBL296086 100754 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 487 8 2 8 5.1 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1OC 10.1016/s0960-894x(00)00318-8
44293305 100978 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 100978 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293071 101117 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 101117 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293165 101210 0 None 7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 101210 0 None 7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44341080 110076 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL325417 110076 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293347 162549 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 162549 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293617 188080 0 None 23 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 188080 0 None 23 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432643 146222 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 146222 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293100 186673 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 485 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc(C(C)O)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49276 186673 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 485 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc(C(C)O)c1 10.1016/s0960-894x(00)00318-8
44561368 176230 0 None 42 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176230 0 None 42 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44432636 86943 0 None 8 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 86943 0 None 8 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44432655 148942 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394634 148942 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11583756 189052 0 None 31 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL515123 189052 0 None 31 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
11712618 179636 0 None 22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 179636 0 None 22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
25194091 188413 0 None 13 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 188413 0 None 13 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44214108 100634 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 100634 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
145952498 162314 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 719 14 2 10 4.8 COc1ccccc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
CHEMBL4173316 162314 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 719 14 2 10 4.8 COc1ccccc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
44321148 96347 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265042 96347 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321509 204458 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86431 204458 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44292874 183248 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48069 183248 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
10187208 66400 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185785 66400 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44434386 89364 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL237734 89364 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434391 89643 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 926 27 2 16 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238177 89643 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 926 27 2 16 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44293015 174455 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 530 7 4 5 6.6 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL45675 174455 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 530 7 4 5 6.6 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
44432648 149682 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 149682 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451356 95903 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL261649 95903 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44293129 181144 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47772 181144 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
22129998 100792 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100792 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44572236 171323 0 None -6 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171323 0 None -6 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293264 100731 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295908 100731 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
16148338 161387 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL415573 161387 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10649568 14382 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Functional antagonism at the rhesus monkey gonadotropin-releasing hormone receptorFunctional antagonism at the rhesus monkey gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Functional antagonism at the rhesus monkey gonadotropin-releasing hormone receptorFunctional antagonism at the rhesus monkey gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44321290 204670 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87785 204670 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44432654 159236 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 159236 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
9961721 167903 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167903 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
16144832 161218 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414061 161218 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10231401 1981 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
5584 1981 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
CHEMBL314260 1981 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
44572235 188907 0 None 5 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188907 0 None 5 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44340888 110023 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL325091 110023 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
44380552 58436 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168655 58436 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44380643 58395 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
CHEMBL168498 58395 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
44361468 161171 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL413698 161171 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147757 161243 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL414266 161243 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16144824 96386 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
CHEMBL265286 96386 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
44361351 160400 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL411565 160400 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361797 161242 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414249 161242 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44293223 173719 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45501 173719 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
9809394 119991 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL354524 119991 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293178 100939 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 100939 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
9809382 100195 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL292291 100195 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434373 89603 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238160 89603 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44292820 100684 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 498 8 3 7 4.4 Cc1cc(CC(N)=O)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295556 100684 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 498 8 3 7 4.4 Cc1cc(CC(N)=O)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44293011 100772 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 563 6 2 6 7.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL296198 100772 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 563 6 2 6 7.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44573791 186795 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 186795 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44215055 100807 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 100807 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293249 184851 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 184851 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44292977 173655 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 173655 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44434415 88085 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 821 18 3 13 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235180 88085 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 821 18 3 13 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434432 88306 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 953 27 3 16 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL236221 88306 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 953 27 3 16 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44215053 185028 0 None 1 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 185028 0 None 1 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293485 101032 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 101032 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44444663 93753 0 None -4 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 93753 0 None -4 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44593415 188780 0 None -20 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188780 0 None -20 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44359287 11515 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 11515 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 11515 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
22100905 183674 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 183674 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44359303 11517 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180760 11517 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141539 11517 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44359285 11507 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 11507 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 11507 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44576656 187653 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 571 10 2 7 4.2 N[C@@H](Cn1c(=O)c(-c2ccc(COCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499588 187653 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 571 10 2 7 4.2 N[C@@H](Cn1c(=O)c(-c2ccc(COCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
138978204 166190 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4283577 166190 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
145992260 166370 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
CHEMBL4286937 166370 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
16147451 96553 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266653 96553 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL2370894 208191 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C[C@@H]3NC(=O)NC3=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16147765 161290 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361477 161290 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414715 161290 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10051739 84994 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL22653 84994 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44321345 204509 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86758 204509 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
10258659 12078 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 12078 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 12078 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293487 101150 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 101150 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145973618 162523 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 635 8 1 8 4.7 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4176683 162523 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 635 8 1 8 4.7 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44380236 58398 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168506 58398 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
16144222 96561 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266728 96561 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44341113 9813 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL114438 9813 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44321411 106513 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315326 106513 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
101755083 1327 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
16136245 1327 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
4379 1327 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
5585 1327 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL415606 1327 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB06699 1327 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
44361587 160752 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
CHEMBL412336 160752 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
9872676 77811 0 None -2 2 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77811 0 None -2 2 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
44321412 204519 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86805 204519 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
16144865 83013 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1648 43 18 18 1.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C(NC(N)=O)NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL219799 83013 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1648 43 18 18 1.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C(NC(N)=O)NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
53239183 162281 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 603 8 1 8 4.3 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172886 162281 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 603 8 1 8 4.3 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
58022331 128121 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2sccc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
CHEMBL3668004 128121 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2sccc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
44292918 170839 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170839 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936667 100039 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL291201 100039 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44432627 147584 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL393540 147584 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
10649568 14382 0 None -4 2 Rat 7.1 pIC50 = 7.1 Functional
Functional antagonism at GnRH receptor in rat (PI turnover)Functional antagonism at GnRH receptor in rat (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None -4 2 Rat 7.1 pIC50 = 7.1 Functional
Functional antagonism at GnRH receptor in rat (PI turnover)Functional antagonism at GnRH receptor in rat (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44293177 174121 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45597 174121 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
10438167 100699 0 None -15 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 100699 0 None -15 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44321695 105488 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313086 105488 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
44292979 187596 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49893 187596 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
11712618 179636 0 None -22 2 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 179636 0 None -22 2 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293151 100692 0 None -23 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 100692 0 None -23 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44560995 178564 0 None -9 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178564 0 None -9 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44434433 88307 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 997 30 3 17 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL236222 88307 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 997 30 3 17 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434436 150428 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395825 150428 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
16221379 161370 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL415380 161370 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
58022131 128124 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 442 5 2 6 4.0 Cc1ccccc1COc1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668007 128124 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 442 5 2 6 4.0 Cc1ccccc1COc1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44432642 153048 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 153048 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432649 86258 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231739 86258 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44359264 11508 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 11508 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 11508 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44185958 154447 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 154447 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
145956692 161512 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 606 9 2 10 3.3 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4160698 161512 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 606 9 2 10 3.3 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44380488 58692 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169238 58692 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
44432652 96680 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 96680 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
16146884 96709 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268146 96709 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44398118 166733 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1632 41 18 19 -0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL429378 166733 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1632 41 18 19 -0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44593424 175549 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175549 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44593424 175549 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175549 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
16156706 136564 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL374747 136564 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16144863 96414 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL265556 96414 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16156706 136564 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL374747 136564 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
11620431 178779 0 None 21 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178779 0 None 21 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
15602807 8121 0 None 8 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8121 0 None 8 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44293485 101032 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 101032 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44292837 100989 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccsc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL297768 100989 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccsc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292683 186364 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 537 7 2 6 7.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(-c4ccccc4)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL49028 186364 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 537 7 2 6 7.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(-c4ccccc4)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293134 186808 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186808 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44432650 86330 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
CHEMBL232097 86330 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
15602806 8197 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8197 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44560995 178564 0 None 9 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178564 0 None 9 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44321147 162916 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL420051 162916 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44293443 183459 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48224 183459 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293511 100803 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 100803 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44444645 154449 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 154449 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44293075 90219 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 90219 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 187595 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 187595 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44434404 166004 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL427981 166004 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44432635 86342 0 None 5 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 86342 0 None 5 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
44295755 192509 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 192509 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 192509 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293486 186824 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 186824 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293222 175377 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL138464 175377 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45883 175377 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44359289 12030 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184180 12030 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL337323 12030 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44361351 160400 0 None - 1 Human 9.5 pKd = 9.5 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL411565 160400 0 None - 1 Human 9.5 pKd = 9.5 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144515 155574 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL406337 155574 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL1251 206909 21 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2370890 208190 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
101755083 1327 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16136245 1327 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
4379 1327 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
5585 1327 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL415606 1327 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB06699 1327 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16146884 96709 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268146 96709 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361587 160752 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
CHEMBL412336 160752 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
16146554 160900 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
CHEMBL412749 160900 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
44361802 168272 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL438018 168272 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
1188 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16131215 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
35 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1252 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB00106 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
44361796 82965 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL219461 82965 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147451 96553 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266653 96553 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361797 161242 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414249 161242 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144824 96386 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
CHEMBL265286 96386 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
16144863 96414 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL265556 96414 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144222 96561 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266728 96561 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361888 141232 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL386105 141232 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44361468 161171 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL413698 161171 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
1190 867 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
25074887 867 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
583 867 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1200490 867 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB00050 867 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16147453 96657 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL267622 96657 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147767 96897 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL269516 96897 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268875 209016 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
9854500 101789 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cellsAntagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
CHEMBL303274 101789 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cellsAntagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
16148338 161387 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL415573 161387 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16146022 169541 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL444381 169541 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL269711 209046 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2105773 210984 7 None -1 2 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL409018 210984 7 None -1 2 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44361795 167922 0 None - 1 Human 8.7 pKd = 8.7 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435322 167922 0 None - 1 Human 8.7 pKd = 8.7 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL262747 208791 8 None 1 2 Human 8.6 pKd = 8.6 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10394119 113936 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Competitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptorCompetitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113936 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Competitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptorCompetitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
1184 3663 31 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 3663 31 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 3663 31 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
145991962 166268 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4285058 166268 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
11583756 189052 0 None 31 2 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL515123 189052 0 None 31 2 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978204 166190 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4283577 166190 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
145992260 166370 0 None - 1 Human 6.8 pKi = 6.8 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
CHEMBL4286937 166370 0 None - 1 Human 6.8 pKi = 6.8 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
145993478 166755 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
CHEMBL4294163 166755 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
1179 945 31 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 945 31 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 945 31 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
145980339 166023 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4280124 166023 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978203 166136 0 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
CHEMBL4282476 166136 0 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
138978207 166589 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
CHEMBL4290761 166589 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
145984647 165852 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4277116 165852 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
3860 731 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
436 731 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
50225 731 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 731 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
DB06719 731 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
3860 731 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
436 731 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
50225 731 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 731 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06719 731 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1177 3794 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
25074470 3794 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
2968 3794 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201334 3794 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06825 3794 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1162 1793 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 1793 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 731 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 731 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 731 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 731 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 731 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
1162 1793 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 1793 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 731 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 731 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 731 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 731 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 731 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11980076 206701 27 None 1 2 Rat 8.1 pIC50 = 8.1 Functional
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 206701 27 None 1 2 Rat 8.1 pIC50 = 8.1 Functional
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
11250647 1510 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
5293 1510 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
8362 1510 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
CHEMBL1208155 1510 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
DB11979 1510 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
10348973 3249 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5432 3249 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5586 3249 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
CHEMBL1800159 3249 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
DB11853 3249 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
1175 2256 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1559 2256 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
657181 2256 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201199 2256 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB00007 2256 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
10348973 3249 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5432 3249 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5586 3249 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
CHEMBL1800159 3249 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
DB11853 3249 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
12784 571 8 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
85469632 571 8 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
CHEMBL4537788 571 8 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
12283 2282 12 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
16656889 2282 12 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
CHEMBL3668014 2282 12 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
11496610 4000 11 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
5582 4000 11 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
CHEMBL474991 4000 11 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
1164 1794 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1164 1794 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17942747
1164 1794 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
5581 1413 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
11496610 4000 11 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
5582 4000 11 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
CHEMBL474991 4000 11 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
1162 1793 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16132914 1793 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1190 867 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
25074887 867 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
583 867 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL1200490 867 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
DB00050 867 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
10231401 1981 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
5584 1981 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
CHEMBL314260 1981 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
101827019 2066 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
16130938 2066 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
3854 2066 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
73952264 2066 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL3989438 2066 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
1175 2256 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1559 2256 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
657181 2256 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
CHEMBL1201199 2256 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
DB00007 2256 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
5583 246 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
10231401 1981 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
10231401 1981 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
5584 1981 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
5584 1981 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
CHEMBL314260 1981 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
CHEMBL314260 1981 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
10348973 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
10348973 3249 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5432 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5432 3249 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5586 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5586 3249 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
CHEMBL1800159 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
CHEMBL1800159 3249 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
DB11853 3249 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
DB11853 3249 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
12394 2445 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 752 12 2 9 6.0 C1CN(CCC21c1c(CO2)n(c(=O)n(c1=O)C[C@@H](c1ccccc1)NCCCC(=O)O)Cc1c(cccc1F)C(F)(F)F)Cc1ccc(o1)C(F)(F)F 26321528
71727383 2445 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 752 12 2 9 6.0 C1CN(CCC21c1c(CO2)n(c(=O)n(c1=O)C[C@@H](c1ccccc1)NCCCC(=O)O)Cc1c(cccc1F)C(F)(F)F)Cc1ccc(o1)C(F)(F)F 26321528
1192 147 41 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
1794 147 41 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
CHEMBL501701 147 41 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
10279142 1589 0 None - 1 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1182 1589 0 None - 1 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1171 3519 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
118856782 3519 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1173 3823 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1172 3801 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16130930 3801 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1169 1770 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
123777 1770 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1162 1793 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
16132914 1793 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1179 945 31 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
9957278 945 31 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
CHEMBL494803 945 31 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
1162 1793 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
16132914 1793 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
1184 3663 31 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
9874838 3663 31 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
CHEMBL71917 3663 31 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
1174 1354 0 None - 1 Mouse 9.9 pIC50 None 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228


Get vendors


Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44348326 96705 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL268095 96705 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
11563584 139005 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 630 10 2 7 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379629 139005 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 630 10 2 7 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10100930 63173 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63173 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388960 63222 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800663 63222 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
11692959 77745 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 612 10 2 7 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210294 77745 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 612 10 2 7 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10348973 3249 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3249 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3249 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3249 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3249 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
53387071 63175 4 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63175 4 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL2370519 208112 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm010112g
53388958 63220 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800661 63220 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389117 63225 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800666 63225 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL414239 161241 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1530 40 18 21 -1.6 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CC/N=C1\C(=O)c2ccccc2C(O)=C1Cl)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
10258719 152695 0 None - 0 Human 10.0 pIC50 = 10 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 650 12 2 10 4.8 CCOCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
CHEMBL3977463 152695 0 None - 0 Human 10.0 pIC50 = 10 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 650 12 2 10 4.8 CCOCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
1185 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
9939837 77482 0 None - 0 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 651 9 2 7 6.6 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL2092994 77482 0 None - 0 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 651 9 2 7 6.6 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9961721 167903 0 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167903 0 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1185 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
3038517 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
CHEMBL22055 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
DB06494 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
44395650 168744 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL441676 168744 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
1185 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3632 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
53386915 63171 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63171 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389115 63223 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800664 63223 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
18324807 63227 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63227 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44293053 101009 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 101009 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292838 101034 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 101034 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 187595 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 187595 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
11700433 77242 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 675 11 1 6 8.5 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)c2ccccc2)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL208812 77242 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 675 11 1 6 8.5 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)c2ccccc2)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11707186 77862 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 1 7 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210709 77862 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 1 7 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
20691661 79188 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79188 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11512905 137877 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137877 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
155524081 170304 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)O[C@@H]1[C@@H](CO)O[C@@H](n2ccc(N)nc2=O)C1(F)F)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4454362 170304 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)O[C@@H]1[C@@H](CO)O[C@@H](n2ccc(N)nc2=O)C1(F)F)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
10371708 63176 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63176 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
44293177 174121 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45597 174121 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
67143119 175271 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585638 175271 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143780 171676 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4474379 171676 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
67143102 172353 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4516712 172353 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143023 174415 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4566719 174415 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9895596 63170 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
CHEMBL1800152 63170 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
1184 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9874838 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
CHEMBL71917 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
1184 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9875078 75561 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 680 11 1 8 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL20511 75561 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 680 11 1 8 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9853275 79416 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 681 11 2 8 6.9 CCONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21217 79416 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 681 11 2 8 6.9 CCONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9831689 98547 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 679 10 2 7 7.4 CC(C)NC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280126 98547 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 679 10 2 7 7.4 CC(C)NC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1184 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9874838 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
CHEMBL71917 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
23656390 161122 0 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
CHEMBL413245 161122 0 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
44321964 95959 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL261979 95959 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
9895596 63170 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63170 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386916 63172 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800154 63172 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386917 63174 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63174 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388959 63221 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccnc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800662 63221 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccnc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389118 63226 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800667 63226 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53386756 63228 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800669 63228 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386757 63229 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
CHEMBL1800670 63229 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
44293348 100013 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100013 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293075 90219 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 90219 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
18914263 96440 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 96440 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44214108 100634 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 100634 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
21254068 101305 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 101305 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293070 165531 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 165531 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914272 169103 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 169103 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
21254089 181065 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 181065 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292988 181849 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 181849 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
18914248 187138 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 187138 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
1184 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
10794239 12938 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL1190107 12938 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL540109 12938 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
9809590 79212 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 6 8.1 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211503 79212 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 6 8.1 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11643195 79404 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 2 7 7.2 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)(C)O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212121 79404 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 2 7 7.2 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)(C)O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11628915 137684 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 2 7 6.5 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CO)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL377015 137684 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 2 7 6.5 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CO)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11512905 137877 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137877 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
1184 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
9874838 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
CHEMBL71917 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
1184 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 3663 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
118074127 175134 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4582367 175134 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44348308 81562 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL216519 81562 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
53387071 63175 4 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63175 4 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44346805 168277 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
91931800 168277 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
CHEMBL438099 168277 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
1175 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
1559 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
657181 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
CHEMBL1201199 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
DB00007 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
145958346 161420 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 543 8 1 7 4.3 COc1ccc(F)cc1C(N)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4159155 161420 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 543 8 1 7 4.3 COc1ccc(F)cc1C(N)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
10100930 63173 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63173 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10985312 78321 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78321 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9896373 98579 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 1 8 7.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(NC(=O)C(C)C)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL280365 98579 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 1 8 7.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(NC(=O)C(C)C)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
44395623 124124 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL364167 124124 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10053165 183407 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL48192 183407 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44321052 204538 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86912 204538 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
44340906 9465 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112400 9465 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
9985901 109951 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL324654 109951 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
1185 3632 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
53386758 63168 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 603 12 3 10 3.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCO)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800150 63168 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 603 12 3 10 3.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCO)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386914 63169 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 12 3 10 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CC(C)(C)O)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800151 63169 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 12 3 10 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CC(C)(C)O)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389116 63224 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 672 11 2 11 4.6 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCn2ccnn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800665 63224 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 672 11 2 11 4.6 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCn2ccnn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
9895596 63170 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63170 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386915 63171 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63171 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10009345 100439 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 642 11 2 8 5.8 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL293921 100439 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 642 11 2 8 5.8 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44380643 58395 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
CHEMBL168498 58395 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
44380625 58403 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168538 58403 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
10008768 58411 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168563 58411 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380488 58692 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169238 58692 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
9894997 119795 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352806 119795 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44214098 100811 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296483 100811 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293443 183459 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48224 183459 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293148 186893 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49412 186893 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936150 188140 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50500 188140 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293054 101012 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 101012 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292977 173655 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 173655 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
1175 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
1559 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
657181 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
DB00007 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
44348321 96068 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1520 39 15 17 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)c2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262825 96068 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1520 39 15 17 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)c2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348306 156439 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407316 156439 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348399 160766 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL412472 160766 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348528 161366 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL415351 161366 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
10053165 183407 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/s0960-894x(00)00318-8
CHEMBL48192 183407 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/s0960-894x(00)00318-8
10053165 183407 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL48192 183407 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
9961721 167903 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167903 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1175 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
1559 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
657181 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
DB00007 2256 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
67144164 173304 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
CHEMBL4539811 173304 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
9961721 167903 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44395435 123282 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362371 123282 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
67143710 169757 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447139 169757 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10348973 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
10348973 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3249 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
87285473 173508 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4544693 173508 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145955571 162097 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 162097 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
10348973 3249 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3249 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3249 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3249 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3249 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
67144353 171647 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474058 171647 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145954246 161846 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 529 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4165983 161846 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 529 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44348533 161179 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL413752 161179 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm970024p
67143773 169927 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449450 169927 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143621 170727 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4460880 170727 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
87285554 172748 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526641 172748 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9917618 98176 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 653 9 3 8 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NO)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
CHEMBL277214 98176 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 653 9 3 8 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NO)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
10919567 98560 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280213 98560 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44321963 105448 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
CHEMBL312864 105448 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
44321411 106513 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315326 106513 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321345 204509 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86758 204509 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
44293163 188105 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188105 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44341082 9670 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113574 9670 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44341046 9966 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL115365 9966 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44340888 110023 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL325091 110023 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
1185 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
9895731 201737 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 644 11 2 9 5.4 CONC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL65769 201737 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 644 11 2 9 5.4 CONC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
9873212 57257 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166649 57257 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
9938925 57272 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166763 57272 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380626 58404 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168539 58404 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380537 96100 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL263004 96100 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44380394 119430 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL349638 119430 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380514 119694 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352051 119694 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
9809394 119991 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL354524 119991 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44292940 100781 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296244 100781 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293651 162552 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417726 162552 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293335 172048 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172048 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293349 183532 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48273 183532 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
10258643 100900 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297151 100900 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293178 100939 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 100939 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293074 187190 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 187190 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
11614283 77756 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 627 11 1 6 7.9 CCC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210321 77756 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 627 11 1 6 7.9 CCC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11592777 138710 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 2 6 8.0 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL378979 138710 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 2 6 8.0 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44413067 138757 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 593 11 1 7 6.9 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379198 138757 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 593 11 1 7 6.9 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44352512 116783 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
CHEMBL339636 116783 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
67143509 169487 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4443108 169487 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44348324 156724 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407681 156724 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44309572 202626 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
CHEMBL71561 202626 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
10649568 14382 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL120432 14382 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
87285768 169917 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169917 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10649568 14382 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of binding to GnRH receptor in humanIn vitro inhibition of binding to GnRH receptor in human
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of binding to GnRH receptor in humanIn vitro inhibition of binding to GnRH receptor in human
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
10649568 14382 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
CHEMBL120432 14382 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
67142732 169045 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436854 169045 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145949496 162296 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 162296 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL2370593 208121 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](N)C(N)=O)cc1 10.1021/jm970024p
44460342 167348 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL431402 167348 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
18324807 63227 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63227 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
1185 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
10649568 14382 0 None 10 2 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkeyIn vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkey
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None 10 2 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkeyIn vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkey
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
9809382 100195 0 None - 1 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL292291 100195 0 None - 1 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44380538 58761 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169620 58761 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293591 101112 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101112 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293129 181144 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47772 181144 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293213 187208 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49590 187208 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293071 101117 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 101117 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293366 161650 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 161650 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
1175 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1559 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
657181 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
DB00007 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL2370590 208119 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
44293205 183369 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 643 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)ccc1I 10.1016/s0960-894x(00)00318-8
CHEMBL48165 183369 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 643 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)ccc1I 10.1016/s0960-894x(00)00318-8
44295699 100738 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL295948 100738 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
9828888 101342 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL300295 101342 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
1175 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
1559 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
657181 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
DB00007 2256 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
44348325 96148 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](NC(=O)c2ccc(NC(C)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263358 96148 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](NC(=O)c2ccc(NC(C)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370592 208120 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CC(C)C)cc1 10.1021/jm970024p
44395462 167649 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL433594 167649 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10371708 63176 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63176 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
155531714 175607 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175607 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
58239302 161429 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 161429 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11167850 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1178 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1187 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL179691 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11167850 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
1178 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
1187 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL179691 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44348454 156666 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407615 156666 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
1184 3663 31 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9874838 3663 31 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
CHEMBL71917 3663 31 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9896737 82940 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 695 11 2 8 7.3 CC(C)ONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21936 82940 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 695 11 2 8 7.3 CC(C)ONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9893269 65949 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL184819 65949 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10187208 66400 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185785 66400 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395533 66450 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185986 66450 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10231401 1981 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
5584 1981 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
CHEMBL314260 1981 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
44321148 96347 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265042 96347 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44320895 163699 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL421160 163699 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
44321393 204537 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86911 204537 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
44340928 9637 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113432 9637 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
44340929 112990 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL332049 112990 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
67143618 169716 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446435 169716 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9960399 50256 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL157412 50256 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380512 57117 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165456 57117 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380236 58398 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168506 58398 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44380796 58876 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170159 58876 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44380798 58999 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170606 58999 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380536 119872 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353395 119872 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44293273 161531 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL416102 161531 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293592 162328 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162328 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44292918 170839 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170839 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293134 186808 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186808 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293411 188172 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50552 188172 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44412890 77892 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 607 11 1 7 7.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210888 77892 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 607 11 1 7 7.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44295753 186154 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL48879 186154 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
44348453 96659 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
CHEMBL267642 96659 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
44348316 96070 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262842 96070 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348148 156197 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407058 156197 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348527 161272 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414558 161272 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370594 208122 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C(N)=O)N(C)C=O)cc1 10.1021/jm970024p
87285708 173323 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4540232 173323 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155517188 169585 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4444427 169585 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
44395502 165334 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL424991 165334 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
9808288 110980 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL327704 110980 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321498 204572 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87099 204572 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44341197 108535 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL321258 108535 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
44341198 112546 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL331144 112546 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
44460343 203624 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL79639 203624 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
11167850 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44305285 100138 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 630 11 2 9 5.0 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NOC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL291896 100138 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 630 11 2 9 5.0 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NOC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
44380478 58432 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168637 58432 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
44380483 58751 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169569 58751 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
9808288 110980 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL327704 110980 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
44380513 119673 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL351836 119673 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44292919 100663 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100663 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293650 161767 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL416470 161767 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293045 185232 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 7 5.7 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc4c(c3)CCC4)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48674 185232 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 7 5.7 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc4c(c3)CCC4)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293206 186596 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1ccc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL49230 186596 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1ccc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
145955844 162130 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 7 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(C)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4170478 162130 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 7 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(C)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44348534 161265 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
91935482 161265 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414469 161265 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348307 161264 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414468 161264 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44395491 123319 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362544 123319 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44321412 204519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86805 204519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321290 204670 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87785 204670 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44341164 9458 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112378 9458 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
44341056 114023 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL333614 114023 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL None None None None 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
53386917 63174 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63174 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
71449058 83971 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 83971 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 83971 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380222 57276 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166778 57276 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293605 100691 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295591 100691 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44292874 183248 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48069 183248 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
1175 2256 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1559 2256 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
657181 2256 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 2256 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
DB00007 2256 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1175 2256 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
1559 2256 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
657181 2256 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 2256 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
DB00007 2256 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
44348056 159459 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL410798 159459 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348400 168117 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436683 168117 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44395583 123814 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL363663 123814 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44341113 9813 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL114438 9813 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44341199 112547 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL331145 112547 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
9961721 167903 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
11167850 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44295755 192509 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 192509 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 192509 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380681 58451 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168726 58451 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380147 119759 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352566 119759 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
20691661 79188 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79188 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44348057 95997 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262309 95997 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370589 208118 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CN[C@@H](NC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm970024p
44293222 175377 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL138464 175377 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45883 175377 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44295755 192509 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2111956 192509 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL52278 192509 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
67143518 174292 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4563562 174292 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
87285476 170891 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4463476 170891 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11017929 98551 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 624 9 1 8 6.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(N)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL280170 98551 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 624 9 1 8 6.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(N)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
10930638 98559 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
CHEMBL280212 98559 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
44321101 96387 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265288 96387 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321394 106443 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
CHEMBL314860 106443 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
44321410 106512 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315325 106512 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
87285565 169691 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446131 169691 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143755 174843 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4576169 174843 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9961721 167903 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44293377 101420 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 101420 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293347 162549 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 162549 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44412945 96245 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 7 7.8 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL264121 96245 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 7 7.8 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44293386 174949 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL45784 174949 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
67143613 170449 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456703 170449 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
22129998 100792 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100792 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL None None None None 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
87285570 170165 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4452347 170165 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143804 172615 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4522657 172615 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285767 174295 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4563686 174295 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9961721 167903 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44380146 119758 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352565 119758 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44380318 119860 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353308 119860 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44380487 167007 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL430069 167007 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
44292950 161883 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL416651 161883 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292868 176323 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46177 176323 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
67143547 170940 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464132 170940 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44320921 106672 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316362 106672 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67143761 170785 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4461692 170785 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285550 173746 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4550720 173746 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293555 100727 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295897 100727 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44348297 166895 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL429902 166895 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
145953172 161910 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(Cl)cc(Cl)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167067 161910 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(Cl)cc(Cl)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL415547 211431 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
67143505 171654 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 601 8 1 8 4.6 Cc1c(N2CCN(Cc3cccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474116 171654 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 601 8 1 8 4.6 Cc1c(N2CCN(Cc3cccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44321146 105911 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313946 105911 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209233 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3632 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3632 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3632 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL415547 211431 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44395677 66390 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185738 66390 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44293249 184851 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL48616 184851 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321509 204458 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86431 204458 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44359285 11507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 11507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 11507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293249 184851 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 184851 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44215053 185028 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 185028 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44348149 168142 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436897 168142 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
67143570 171181 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467407 171181 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
23656390 161122 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
CHEMBL413245 161122 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
11167850 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL None None None None 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67142962 173994 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 629 9 1 8 4.6 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4556717 173994 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 629 9 1 8 4.6 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44380797 58965 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170499 58965 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44215055 100807 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 100807 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44593425 176181 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
CHEMBL460480 176181 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
11167850 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3632 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3632 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3632 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
70689073 77258 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
91900370 77258 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2088253 77258 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
155531714 175607 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175607 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
10231401 1981 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
5584 1981 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
CHEMBL314260 1981 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
44593425 176181 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 176181 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
44593425 176181 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176181 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
11167850 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
67144370 174033 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4557575 174033 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44293488 101071 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 101071 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293376 101192 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 101192 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44348172 155199 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1547 39 14 17 1.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(C)=O)cc1 10.1021/jm970024p
CHEMBL405736 155199 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1547 39 14 17 1.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(C)=O)cc1 10.1021/jm970024p
44402640 161269 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
CHEMBL414514 161269 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
11167850 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
87285770 175460 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
CHEMBL4590493 175460 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
11620431 178779 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178779 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44359264 11508 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 11508 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 11508 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293802 101549 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 101549 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293081 182112 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL47895 182112 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402639 154678 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL402671 154678 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
164628446 185720 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assayDisplacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assay
ChEMBL 1627 43 20 26 -5.2 CC(C)CC(NC(=O)C(CCCCNC(=O)/C=N/OCC(=O)OCC1OC(n2ccc(N)nc2=O)C(F)(F)C1O)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1cc2ccccc2[nH]1)NC(=O)C(Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCNC(=N)N)C(=O)N1CCCC1C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113018
CHEMBL4874610 185720 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assayDisplacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assay
ChEMBL 1627 43 20 26 -5.2 CC(C)CC(NC(=O)C(CCCCNC(=O)/C=N/OCC(=O)OCC1OC(n2ccc(N)nc2=O)C(F)(F)C1O)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1cc2ccccc2[nH]1)NC(=O)C(Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCNC(=N)N)C(=O)N1CCCC1C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113018
CHEMBL436874 211931 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL None None None None 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
10438167 100699 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 100699 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44380319 58427 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168615 58427 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44348174 159485 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
CHEMBL410818 159485 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
67143612 170473 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456937 170473 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402639 154678 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL402671 154678 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402518 157968 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL409138 157968 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402640 161269 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
CHEMBL414514 161269 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
91810333 178988 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
CHEMBL4741994 178988 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
118179218 179425 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4747248 179425 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
10004181 100604 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL294910 100604 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
44573110 186601 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 186601 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44573113 192625 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL523711 192625 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
1185 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44577104 178159 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178159 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
67143054 169710 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 581 8 1 7 3.9 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4446360 169710 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 581 8 1 7 3.9 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
53239181 171927 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4483419 171927 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1185 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44305605 201631 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 613 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL64920 201631 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 613 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11214294 121668 0 None 912 2 Human 8.0 pIC50 = 8 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121668 0 None 912 2 Human 8.0 pIC50 = 8 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL438652 212027 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
44293111 100735 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 100735 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
10004181 100604 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL294910 100604 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
15895698 205142 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL90725 205142 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
11980076 206701 27 None - 1 Human 8.0 pIC50 = 8 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 206701 27 None - 1 Human 8.0 pIC50 = 8 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL436874 211931 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL None None None None 10.1021/jm0506928
CHEMBL448249 212195 13 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL436874 211931 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL None None None None 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44359456 12083 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184286 12083 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342908 12083 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44322384 105646 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL313501 105646 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
44365638 41665 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 518 12 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(OCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149441 41665 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 518 12 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(OCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44214104 121229 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 540 10 4 5 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCNCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL358901 121229 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 540 10 4 5 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCNCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44444617 93698 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 93698 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
10930638 98559 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322165 204485 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 458 5 1 4 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(C(F)(F)F)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86609 204485 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 458 5 1 4 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(C(F)(F)F)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
11599857 76510 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 597 11 0 9 6.5 CCOC(=O)c1cn(Cc2ccccc2[N+](=O)[O-])c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL206964 76510 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 597 11 0 9 6.5 CCOC(=O)c1cn(Cc2ccccc2[N+](=O)[O-])c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11520078 79300 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 577 10 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2C#N)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211588 79300 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 577 10 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2C#N)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44365131 38272 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 472 13 3 4 6.5 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL146451 38272 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 472 13 3 4 6.5 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44364998 40197 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 443 11 3 4 5.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148246 40197 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 443 11 3 4 5.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
10808668 204884 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 362 4 1 4 5.2 Oc1nc2cc(Cl)ccc2c(OCc2ccccn2)c1-c1ccccc1 10.1016/s0960-894x(99)00446-1
CHEMBL89086 204884 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 362 4 1 4 5.2 Oc1nc2cc(Cl)ccc2c(OCc2ccccn2)c1-c1ccccc1 10.1016/s0960-894x(99)00446-1
10837806 77657 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 463 7 0 7 5.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(C)c2c1=O 10.1021/jm0512894
CHEMBL209836 77657 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 463 7 0 7 5.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(C)c2c1=O 10.1021/jm0512894
162653870 179951 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753775 179951 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
44406776 133806 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444642 93921 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 93921 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67142732 169045 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436854 169045 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44417615 141379 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67143815 170964 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464440 170964 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143102 172353 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4516712 172353 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71623059 180233 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180233 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44444645 154449 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 154449 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
162673323 182524 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4794864 182524 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
86274853 115674 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
CHEMBL3358414 115674 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
1185 3632 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
67143030 172536 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(F)c3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4520639 172536 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(F)c3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444668 153733 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 153733 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143633 172728 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526188 172728 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL2370265 208070 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1ccccn1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44573275 186822 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493730 186822 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44293151 100692 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 100692 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44293250 101250 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 101250 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
145973124 162460 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 595 8 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(C(F)(F)F)cc3F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4175801 162460 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 595 8 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(C(F)(F)F)cc3F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11167850 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL409218 210996 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N1CCC[C@@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11496945 175891 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175891 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
21899433 154152 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 154152 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44346397 113987 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
1185 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44359193 11518 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180764 11518 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141750 11518 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44402335 71257 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196337 71257 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402468 132286 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370144 132286 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
70697569 77605 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL2096778 77605 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11720984 63134 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL179885 63134 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
162645007 178871 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44346398 14354 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141074 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113231 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
15462666 96042 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96042 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391541 65245 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183237 65245 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391525 165802 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL427500 165802 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365375 120989 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 9 3 2 5.8 Oc1ccc(CCCCNCCc2c(-c3ccc(F)cc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL358416 120989 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 9 3 2 5.8 Oc1ccc(CCCCNCCc2c(-c3ccc(F)cc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
11619758 172633 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 470 6 3 5 5.0 S=c1[nH]c2cccc(OCCN3CCN(c4cccc5[nH]c(-c6ccccc6)nc45)CC3)c2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452293 172633 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 470 6 3 5 5.0 S=c1[nH]c2cccc(OCCN3CCN(c4cccc5[nH]c(-c6ccccc6)nc45)CC3)c2[nH]1 10.1016/j.bmc.2008.05.024
162645007 178871 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
67144335 169260 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 658 9 1 9 4.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439926 169260 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 658 9 1 9 4.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
118179127 182622 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
CHEMBL4795998 182622 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
44444676 154387 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 154387 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444641 154418 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 154418 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143413 169039 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4436711 169039 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
44365877 118962 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 13 3 6 6.2 CCCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL345297 118962 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 13 3 6 6.2 CCCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44573789 186747 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493167 186747 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
11496610 4000 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4000 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4000 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
11532637 7618 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7618 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
53238728 170097 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 545 8 1 7 3.7 Cc1c(N2CCN(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4451627 170097 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 545 8 1 7 3.7 Cc1c(N2CCN(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11496610 4000 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4000 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4000 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
1185 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44391752 161101 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL413062 161101 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
1185 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL None None None None 10.1021/jm0506928
87285476 170891 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4463476 170891 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL436874 211931 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL None None None None 10.1021/jm0506928
44573278 186854 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL493932 186854 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44573628 192604 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL523527 192604 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
25194091 188413 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 188413 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
25193797 189063 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 189063 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
1185 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44267232 9511 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 454 10 3 3 6.0 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
CHEMBL11263 9511 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 454 10 3 3 6.0 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
44402647 69471 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL193740 69471 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
11525693 69472 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193749 69472 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
11237922 65174 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11237922 65174 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183066 65174 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183066 65174 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
25194092 189274 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 6 3 5 5.6 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)c(C)c1 10.1016/j.bmc.2008.05.024
CHEMBL516934 189274 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 6 3 5 5.6 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)c(C)c1 10.1016/j.bmc.2008.05.024
44417614 141074 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391541 65245 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183237 65245 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
87285767 174295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4563686 174295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 2691 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44267270 10265 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 450 9 2 1 7.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc3c(c2)CCCC3)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11623 10265 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 450 9 2 1 7.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc3c(c2)CCCC3)c1 10.1016/s0960-894x(01)00133-0
162652474 179859 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4752711 179859 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
67144367 169284 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 454 6 1 6 3.3 Cc1c(N2CCCCC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4440296 169284 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 454 6 1 6 3.3 Cc1c(N2CCCCC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
87285768 169917 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169917 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162650892 179639 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179639 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
10930638 98559 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44406776 133806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
67144085 170594 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccccc3[N+](=O)[O-])CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4458877 170594 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccccc3[N+](=O)[O-])CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44406776 133806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67144307 172448 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 546 8 1 8 3.1 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4518726 172448 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 546 8 1 8 3.1 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44365486 38867 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3cccc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146921 38867 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3cccc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL329807 209564 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL408737 210971 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44402467 170079 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL445143 170079 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
44402647 69471 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL193740 69471 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
44365119 119132 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 9 3 2 5.7 Oc1ccc(CCCCNCCc2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL346852 119132 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 9 3 2 5.7 Oc1ccc(CCCCNCCc2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
25194090 188331 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL507973 188331 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44346398 14354 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322240 204675 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 3 1 4 5.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL87804 204675 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 3 1 4 5.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
44322436 204928 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 4 1 4 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89387 204928 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 4 1 4 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
123549935 178844 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4740379 178844 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
162647697 179269 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4745391 179269 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44444665 93754 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 93754 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL2430899 208705 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
118179265 179921 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 619 5 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753358 179921 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 619 5 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)C2C 10.1021/acs.jmedchem.0c01076
118178983 182839 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4798682 182839 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
44406776 133806 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44328452 95989 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1072 26 9 12 1.9 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNNC(=O)c1cccnc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL262190 95989 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1072 26 9 12 1.9 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNNC(=O)c1cccnc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
53238731 170399 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4456075 170399 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44214070 178584 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 561 13 3 5 6.2 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL47227 178584 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 561 13 3 5 6.2 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44391808 65249 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183274 65249 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67144408 175326 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3ccon3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4587044 175326 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3ccon3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144409 170529 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL4457786 170529 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144509 173547 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 575 9 1 8 3.7 COc1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4546034 173547 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 575 9 1 8 3.7 COc1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
162672599 182415 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4793643 182415 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
44328414 95995 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1028 23 9 10 2.2 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)Nc1ccccc1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL262292 95995 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1028 23 9 10 2.2 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)Nc1ccccc1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44402404 133028 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL371073 133028 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
11237922 65174 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11237922 65174 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183066 65174 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183066 65174 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15462666 96042 4 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96042 4 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141074 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 141379 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322077 204807 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 421 5 1 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc([N+](=O)[O-])ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL88620 204807 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 421 5 1 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc([N+](=O)[O-])ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44322441 205071 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 412 4 1 5 4.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CN(C)CCO2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL90383 205071 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 412 4 1 5 4.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CN(C)CCO2)c1 10.1016/s0960-894x(99)00446-1
44391574 65744 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
CHEMBL183847 65744 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
162667361 181933 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 181933 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162645007 178871 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44322399 204546 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 7 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCCC2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL86955 204546 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 7 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCCC2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
71666542 179757 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4751345 179757 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67143761 170785 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4461692 170785 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3632 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
118179051 179628 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179628 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44322440 111058 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL328063 111058 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
44365626 205205 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 596 11 3 5 6.4 CCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL91146 205205 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 596 11 3 5 6.4 CCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL436874 211931 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL None None None None 10.1021/jm0506928
9918188 154171 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 154171 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
10930638 98559 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44359252 11511 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180715 11511 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139291 11511 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
71461676 79074 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2113717 79074 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44380192 57131 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57131 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
70691931 73825 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023088 73825 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
15895698 205142 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL90725 205142 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
44322166 204532 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 468 5 1 4 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Br)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86897 204532 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 468 5 1 4 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Br)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
20691661 79188 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79188 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
9909560 9766 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11420 9766 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402492 125650 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
CHEMBL364933 125650 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
44391718 65259 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183325 65259 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365093 118743 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 520 9 3 2 7.7 Oc1ccc(CCCCNCCc2c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL343658 118743 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 520 9 3 2 7.7 Oc1ccc(CCCCNCCc2c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
162645007 178871 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL264526 208870 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44560995 178564 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178564 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
10919052 113007 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10930638 98559 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402232 71052 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195920 71052 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402072 71380 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196616 71380 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44561265 172528 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452044 172528 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44560995 178564 0 None - 3 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178564 0 None - 3 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
67143374 171165 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467261 171165 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162645007 178871 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
162675445 182816 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 182816 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
44444647 154450 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 154450 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
71668147 179400 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4746969 179400 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
86275342 115673 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL3358413 115673 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44365793 120851 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 11 4 4 6.4 CCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL358126 120851 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 11 4 4 6.4 CCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL97540 214139 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444635 154154 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 154154 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
145957339 161747 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3c(F)cccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4164508 161747 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3c(F)cccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44572286 180209 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180209 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
10046374 9052 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL11009 9052 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
10046374 9052 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11009 9052 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143780 171676 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4474379 171676 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL436874 211931 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL None None None None 10.1021/jm0506928
44380624 58811 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169873 58811 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
56655880 73824 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023087 73824 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
70689073 77258 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
91900370 77258 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2088253 77258 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL436874 211931 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL None None None None 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44346667 113231 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44267237 97908 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL275287 97908 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402560 71077 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 1 5 5.9 COc1ccc(Cl)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196088 71077 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 1 5 5.9 COc1ccc(Cl)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402468 132286 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370144 132286 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
44402256 135743 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL373340 135743 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
11330164 64857 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182513 64857 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44346398 14354 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113231 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10919052 113007 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
15462666 96042 4 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96042 4 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402426 132223 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL370028 132223 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391849 122426 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360743 122426 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
162673323 182524 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4794864 182524 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
21899433 154152 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 154152 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44406776 133806 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143135 173940 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4555444 173940 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444670 94030 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 94030 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
67144409 170529 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL4457786 170529 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL268720 209008 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44572235 188907 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188907 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
145955182 161850 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 515 8 1 7 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccs3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4166009 161850 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 515 8 1 7 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccs3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44593425 176181 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176181 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143135 173940 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4555444 173940 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44365087 38598 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 452 9 3 2 7.0 Oc1ccc(CCCCNCCc2c(-c3cc(Cl)cc(Cl)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146693 38598 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 452 9 3 2 7.0 Oc1ccc(CCCCNCCc2c(-c3cc(Cl)cc(Cl)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
67143397 171570 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 9 2 8 3.9 CNC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4473168 171570 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 9 2 8 3.9 CNC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
10074296 9283 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
CHEMBL11149 9283 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
44444642 93921 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 93921 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
10074296 9283 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11149 9283 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
10074296 9283 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11149 9283 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
44402469 71319 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196439 71319 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
44402463 126989 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL366236 126989 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
11720984 63134 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL179885 63134 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11330164 64857 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182513 64857 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365280 120610 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(C)c1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL357622 120610 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(C)c1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
44346667 113231 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44348265 166736 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL429381 166736 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
118167818 178842 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 178842 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
44444639 154416 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 154416 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
44444672 168825 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 168825 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
118178986 181607 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
CHEMBL4782882 181607 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
44444639 154416 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 154416 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
67143773 169927 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449450 169927 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444652 94053 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 94053 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
162651368 179746 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 533 4 1 3 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(C(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4751238 179746 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 533 4 1 3 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(C(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
162660654 180708 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4762368 180708 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
118179218 179425 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4747248 179425 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44593425 176181 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
CHEMBL460480 176181 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
11634198 186773 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 186773 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44573111 187004 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494738 187004 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44593425 176181 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 176181 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
11634198 186773 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmc.2012.09.013
CHEMBL493344 186773 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmc.2012.09.013
44293591 101112 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101112 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
71449141 79073 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 483 7 2 6 6.5 CC[C@H]1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c([N+](=O)[O-])cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL2113716 79073 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 483 7 2 6 6.5 CC[C@H]1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c([N+](=O)[O-])cc23)N1 10.1016/j.bmcl.2003.12.101
11525693 69472 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193749 69472 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211931 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL None None None None 10.1021/jm0506928
67143815 170964 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464440 170964 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
70691931 73825 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023088 73825 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL3085508 209233 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44402335 71257 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196337 71257 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402273 139730 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 456 7 1 7 5.8 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL380576 139730 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 456 7 1 7 5.8 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391771 165458 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL425524 165458 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL405438 155172 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligandAbility to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligand
ChEMBL 1820 46 20 18 5.7 C=CC1=C(C)c2cc1cc1[nH]c(cc3nc(cc4[nH]c(c2)c(C=C)c4C)C(C)=C3CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2CCC(=O)N2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)C2CC[C@@H](C(=O)NCC(N)=O)N2)c(CCC(=O)O)c1C 10.1021/jm020535y
44417615 141379 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162653870 179951 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753775 179951 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
11167850 2691 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
162652474 179859 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4752711 179859 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
87285770 175460 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
CHEMBL4590493 175460 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
44444673 93834 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 93834 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL436874 211931 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL None None None None 10.1021/jm0506928
44573790 192649 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
CHEMBL523849 192649 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
44402469 71319 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196439 71319 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
67142711 171447 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccccc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4471620 171447 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccccc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
145957680 161536 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3C(F)(F)F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4161096 161536 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3C(F)(F)F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44417614 141074 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44359200 12084 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184288 12084 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL343040 12084 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44388018 60137 0 None 389 2 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60137 0 None 389 2 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44402649 97721 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL274002 97721 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
145948913 166914 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1276 29 16 15 -1.9 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCC1 10.1039/C5MD00259A
CHEMBL4299455 166914 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1276 29 16 15 -1.9 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCC1 10.1039/C5MD00259A
44365485 121000 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 435 9 3 3 6.2 Oc1ccc(CCCCNCCc2c(-c3cccc4cnccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL358524 121000 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 435 9 3 3 6.2 Oc1ccc(CCCCNCCc2c(-c3cccc4cnccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
15462666 96042 4 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96042 4 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 14354 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 14354 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402426 132223 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL370028 132223 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391849 122426 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360743 122426 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44391670 64346 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
CHEMBL181864 64346 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
1185 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL None None None None 10.1021/jm0506928
67143613 170449 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456703 170449 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44185958 154447 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 154447 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
10077523 122186 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL360429 122186 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395463 126241 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL365366 126241 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380512 57117 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Compound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assayCompound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assay
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165456 57117 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Compound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assayCompound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assay
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
11980076 206701 27 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm990433g
CHEMBL1007 206701 27 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm990433g
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44444632 93871 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250569 93871 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
67143374 171165 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467261 171165 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144466 175197 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4583933 175197 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10032223 12082 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 12082 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 12082 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
18914263 96440 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 96440 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293264 100731 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295908 100731 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44214069 100835 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL296644 100835 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292838 101034 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 101034 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
21254068 101305 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 101305 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293076 101338 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300268 101338 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293070 165531 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 165531 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914272 169103 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 169103 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
21254089 181065 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 181065 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44413066 77981 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 579 10 1 7 6.5 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211098 77981 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 579 10 1 7 6.5 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44412947 96300 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 608 10 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N(C)C(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL264574 96300 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 608 10 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N(C)C(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
1184 3663 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3663 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3663 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
44348572 96839 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL269097 96839 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348571 159461 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL410799 159461 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44292869 176438 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL46312 176438 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44296258 101141 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCC(C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL298937 101141 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCC(C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
1184 3663 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3663 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3663 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
44321100 106596 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315909 106596 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
9961721 167903 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44380552 58436 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168655 58436 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44380317 167913 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL435262 167913 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL3085508 209233 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL None None None None 10.1021/jm0506928
44293485 101032 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 101032 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44402518 157968 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL409138 157968 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
1185 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
15602805 8008 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8008 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
145962692 161694 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4163619 161694 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44359287 11515 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 11515 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 11515 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293348 100013 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100013 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293486 186824 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 186824 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44292939 100919 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297269 100919 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402395 168515 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL439879 168515 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
155569451 175624 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1711 48 21 25 -3.8 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4593899 175624 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1711 48 21 25 -3.8 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL436874 211931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44380212 57298 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166843 57298 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44348535 159866 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 39 14 17 2.0 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
CHEMBL411144 159866 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 39 14 17 2.0 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
CHEMBL407619 210914 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NCC(=O)n2cc(C)c(=O)[nH]c2=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
1185 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL None None None None 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44402395 168515 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL439879 168515 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL407619 210914 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NCC(=O)n2cc(C)c(=O)[nH]c2=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
87285521 174437 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567165 174437 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44321147 162916 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL420051 162916 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209233 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
53239615 175282 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccco3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585969 175282 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccco3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL None None None None 10.1021/jm0506928
44359458 12026 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 12026 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 12026 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
10345138 122029 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122029 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122029 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
44293335 172048 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172048 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293487 101150 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 101150 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293803 188285 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 188285 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44402398 96518 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL266420 96518 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
87285768 169917 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assayAntagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169917 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assayAntagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL None None None None 10.1021/jm0506928
67143420 162346 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4173938 162346 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44359471 12077 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 12077 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 12077 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
162649425 179430 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4747322 179430 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
86275345 181478 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 181478 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
10897903 79350 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 0 8 7.2 CCC(=O)N(C)c1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21185 79350 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 0 8 7.2 CCC(=O)N(C)c1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274227 98423 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 654 10 0 9 6.8 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc([N+](=O)[O-])cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL279223 98423 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 654 10 0 9 6.8 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc([N+](=O)[O-])cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
44274247 98922 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL282679 98922 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
15895695 106458 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL314963 106458 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44365771 119066 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 541 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL346195 119066 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 541 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL96693 214132 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCN)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573628 192604 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL523527 192604 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
44417614 141074 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67142907 169781 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447551 169781 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10930638 98559 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44305306 100137 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 661 11 1 8 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL291893 100137 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 661 11 1 8 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
9984259 109999 0 None 281 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 109999 0 None 281 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44391752 161101 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL413062 161101 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
145958486 161622 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 541 8 1 7 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(SC)cc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4162543 161622 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 541 8 1 7 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(SC)cc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44365459 98338 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 7 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL278496 98338 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 7 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365399 119155 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL347121 119155 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365457 168091 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 426 10 3 2 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL436414 168091 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 426 10 3 2 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44274228 98208 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(Cl)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277436 98208 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(Cl)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274229 98240 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(Cl)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277653 98240 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(Cl)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274475 98682 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2OC)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL281167 98682 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2OC)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44346397 113987 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322442 112245 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 5 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL330524 112245 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 5 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44322433 204934 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 5 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89443 204934 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 5 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCN2C)c1 10.1016/s0960-894x(99)00446-1
11692806 79391 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212051 79391 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11606766 79425 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccccc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212207 79425 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccccc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11512905 137877 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137877 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44267059 8401 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 503 12 3 3 6.4 CCS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL10941 8401 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 503 12 3 3 6.4 CCS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267091 9693 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 453 10 3 2 6.6 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11370 9693 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 453 10 3 2 6.6 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267250 9065 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11021 9065 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44267233 9797 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11436 9797 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44402589 124639 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL364510 124639 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
44391826 64536 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
CHEMBL182178 64536 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
44391566 65265 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183376 65265 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
9961721 167903 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167903 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44365169 40191 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 458 12 3 4 6.1 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148244 40191 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 458 12 3 4 6.1 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365616 41117 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149004 41117 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365617 42318 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 460 11 4 5 4.7 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)CCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL150041 42318 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 460 11 4 5 4.7 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)CCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
3823 49936 38 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49936 38 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49936 38 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
90663999 106334 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 709 12 3 10 3.4 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1C(=O)OCc1ccccc1 10.1021/jm00129a003
CHEMBL3144570 106334 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 709 12 3 10 3.4 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1C(=O)OCc1ccccc1 10.1021/jm00129a003
44346667 113231 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44346397 113987 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10624976 21398 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm0512894
CHEMBL131751 21398 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm0512894
11592473 77665 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 568 11 1 8 6.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNCc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL209880 77665 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 568 11 1 8 6.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNCc3ccccc3)c2c1=O 10.1021/jm0512894
44348358 140935 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL384385 140935 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44391574 65744 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
CHEMBL183847 65744 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
10624976 21398 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm9803673
CHEMBL131751 21398 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm9803673
44365172 42438 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 8 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL150150 42438 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 8 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44406776 133806 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67142907 169781 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447551 169781 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179174 181884 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4786609 181884 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
85469632 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
CHEMBL4537788 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
118179135 181426 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 181426 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
44321458 105472 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313004 105472 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11618517 186963 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
CHEMBL494554 186963 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
44573670 187090 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)s1 10.1016/j.bmcl.2009.02.043
CHEMBL495174 187090 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)s1 10.1016/j.bmcl.2009.02.043
11712618 179636 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 179636 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44402403 71170 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196288 71170 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
44402649 97721 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL274002 97721 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
44406776 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
10919052 113007 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113231 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44267255 97683 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL273725 97683 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402670 71599 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197317 71599 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
44402673 132734 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL370414 132734 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391516 64027 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL181301 64027 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44417615 141379 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402405 140773 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 395 7 1 5 5.3 COc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL383393 140773 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 395 7 1 5 5.3 COc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391613 167701 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
CHEMBL433954 167701 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
44593415 188780 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188780 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
67143509 169487 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4443108 169487 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143490 171033 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4465381 171033 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144353 171647 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474058 171647 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285495 171576 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)n3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4473194 171576 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)n3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267258 96912 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL269636 96912 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL413854 161189 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Ability to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligandAbility to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligand
ChEMBL 1810 46 21 19 4.4 C=CC1=C(C)c2cc1cc1[nH]c(cc3nc(cc4[nH]c(c2)c(C=C)c4C)C(C)=C3CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2CCC(=O)N2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)C2CC[C@@H](C(=O)NCC(N)=O)N2)c(CCC(=O)O)c1C 10.1021/jm020535y
91810333 178988 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
CHEMBL4741994 178988 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
11619461 187092 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL495183 187092 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
10930638 98559 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391808 65249 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183274 65249 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2430897 208703 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCCCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
56655880 73824 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023087 73824 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
25193700 172701 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 172701 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10930638 98559 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44348055 168432 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL439258 168432 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44267042 9299 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 517 12 3 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)C(C)C)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11156 9299 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 517 12 3 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)C(C)C)cc2)c1 10.1016/s0960-894x(01)00134-2
44391516 64027 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL181301 64027 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL409979 211035 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None C[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)OCC1c2ccccc2-c2ccccc21)C(N)=O 10.1021/jm990433g
71623059 180233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44406776 133806 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
155538326 171802 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3ccnc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4476330 171802 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3ccnc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162656174 180282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4757424 180282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44406776 133806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2370263 208069 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44573713 192277 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL522202 192277 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
9961721 167903 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359419 12090 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184330 12090 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL344688 12090 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293592 162328 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162328 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44402471 134685 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL372316 134685 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44402645 168547 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL440212 168547 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
44406776 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143621 170727 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4460880 170727 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
44406776 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL265010 208879 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44346667 113231 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44391728 65329 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183430 65329 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391784 121799 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL359860 121799 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44346667 113231 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
86274853 115674 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
CHEMBL3358414 115674 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
44215908 93781 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 93781 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
118178976 180589 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4761024 180589 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
24825725 192017 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 192017 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
24825725 192017 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192017 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44572287 180211 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 180211 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
1185 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
1185 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293343 161651 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 545 12 4 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL416286 161651 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 545 12 4 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44406776 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67144582 175123 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4582222 175123 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
1185 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44417615 141379 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
1185 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44346397 113987 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113231 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44402499 69465 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
CHEMBL193689 69465 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
44391714 121608 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL359668 121608 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL4564312 212249 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHR
ChEMBL None None None O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 nan
44346667 113231 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
1185 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
10208964 66334 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185438 66334 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
86275345 181478 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 181478 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44444617 93698 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 93698 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
71666685 182122 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4789613 182122 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
86275343 182899 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4799511 182899 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44322432 204945 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 427 6 2 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL89501 204945 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 427 6 2 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCN2)c1 10.1016/s0960-894x(99)00447-3
44365628 38682 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 554 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL146762 38682 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 554 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL264501 208867 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44365458 41613 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 8 3 2 5.9 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL149387 41613 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 8 3 2 5.9 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
87285565 169691 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446131 169691 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11619461 187092 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL495183 187092 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
44402072 71380 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196616 71380 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391566 65265 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183376 65265 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365251 38323 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3cc4ccccc4s3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146484 38323 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3cc4ccccc4s3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44214066 167761 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3ccc4ccccc4c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL434318 167761 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3ccc4ccccc4c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44348357 96134 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
77068809 96134 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263200 96134 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
162670223 181979 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4787856 181979 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
162650892 179639 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179639 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573112 187005 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494739 187005 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
11583756 189052 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 189052 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
9961721 167903 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10930638 98559 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL436874 211931 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL2430898 208704 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
67143119 175271 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585638 175271 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402470 140587 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 437 8 1 6 5.5 COc1ccc(C(C)=O)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL382747 140587 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 437 8 1 6 5.5 COc1ccc(C(C)=O)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391835 165740 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL427146 165740 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11167850 2691 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44346397 113987 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
87285554 172748 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526641 172748 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL436874 211931 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL None None None None 10.1021/jm0506928
118178983 182839 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4798682 182839 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
85469632 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
CHEMBL4537788 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
118167818 178842 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 178842 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
44365919 120532 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 597 12 4 6 4.9 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(CC(N)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL356890 120532 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 597 12 4 6 4.9 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(CC(N)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44573626 186939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494416 186939 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
44573627 192250 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL522188 192250 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
44406776 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444628 93870 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 93870 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
12784 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
9979079 8264 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10931 8264 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
9979079 8264 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL10931 8264 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
44402472 132287 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370145 132287 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44406776 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44380192 57131 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57131 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
118074127 175134 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4582367 175134 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285473 173508 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4544693 173508 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267251 98013 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 398 9 2 3 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cncnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL275920 98013 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 398 9 2 3 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cncnc2)c1 10.1016/s0960-894x(01)00133-0
44402589 124639 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL364510 124639 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
44391612 63153 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL179977 63153 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44444663 93753 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 93753 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44406776 133806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
87285768 169917 1 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169917 1 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179051 179628 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179628 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL385022 210584 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL405176 210790 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11604354 186931 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 186931 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
9961721 167903 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359331 12020 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184148 12020 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL334904 12020 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44267036 9573 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 482 11 4 2 6.7 CCNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11299 9573 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 482 11 4 2 6.7 CCNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44402256 135743 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL373340 135743 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
67143633 172728 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526188 172728 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44406776 133806 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL93608 214119 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None C[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm990433g
44348298 81124 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL216112 81124 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44402431 71054 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 440 8 1 7 5.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195924 71054 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 440 8 1 7 5.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402378 69318 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL193529 69318 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402553 71074 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196079 71074 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
44402057 71579 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL197254 71579 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391548 65687 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183698 65687 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391728 65329 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183430 65329 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365250 121331 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 437 9 3 3 6.2 Cn1ccc2cc(-c3[nH]c4ccccc4c3CCNCCCCc3ccc(O)cc3)ccc21 10.1016/s0960-894x(00)00707-1
CHEMBL359001 121331 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 437 9 3 3 6.2 Cn1ccc2cc(-c3[nH]c4ccccc4c3CCNCCCCc3ccc(O)cc3)ccc21 10.1016/s0960-894x(00)00707-1
145948856 166910 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1290 29 16 15 -1.5 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCCC1 10.1039/C5MD00259A
CHEMBL4299432 166910 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1290 29 16 15 -1.5 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCCC1 10.1039/C5MD00259A
118179051 179628 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179628 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573277 186853 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493931 186853 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44346667 113231 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
15602808 8010 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8010 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44406776 133806 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144466 175197 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4583933 175197 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11618517 186963 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
CHEMBL494554 186963 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
11583388 8191 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092626 8191 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44359312 12080 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184274 12080 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342396 12080 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11167850 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44305286 100268 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 611 11 1 8 5.4 C=CC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL292773 100268 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 611 11 1 8 5.4 C=CC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44305362 102198 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 651 11 1 9 6.1 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccoc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL304633 102198 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 651 11 1 9 6.1 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccoc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11167850 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
44380551 58435 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168649 58435 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44293075 90219 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 90219 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44214108 100634 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 100634 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293053 101009 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 101009 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293054 101012 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 101012 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292977 173655 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 173655 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292785 176423 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL46268 176423 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293194 185843 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48763 185843 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
18914248 187138 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 187138 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293074 187190 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 187190 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 187595 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 187595 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44348401 161138 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL413456 161138 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL None None None None 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL None None None None 10.1021/jm0506928
67142985 172299 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3cccc(Cl)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4515452 172299 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3cccc(Cl)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44293484 96255 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL264193 96255 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
44402398 96518 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL266420 96518 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402638 160699 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL411987 160699 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
10258659 12078 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 12078 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 12078 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
22100905 183674 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 183674 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
86275342 115673 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
CHEMBL3358413 115673 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
44341081 167490 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL432450 167490 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL None None None None 10.1021/jm0506928
44293511 100803 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 100803 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
11167850 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL None None None None 10.1021/jm0506928
44572235 188907 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188907 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44402638 160699 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL411987 160699 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL None None None None 10.1021/jm0506928
44359333 11510 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 11510 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 11510 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293617 188080 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 188080 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44380148 119792 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352782 119792 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
11167850 2691 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL None None None None 10.1021/jm0506928
87285732 172373 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4517137 172373 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 209233 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL None None None None 10.1021/jm0506928
67143598 170064 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4451280 170064 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44359191 12085 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 12085 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 12085 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL None None None None 10.1021/jm0506928
44293284 183493 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 8 5.9 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48249 183493 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 8 5.9 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
11478448 65730 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183779 65730 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15462663 98577 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(OC)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280350 98577 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(OC)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44365612 40568 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 610 12 3 5 6.8 CCCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL148571 40568 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 610 12 3 5 6.8 CCCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365627 41384 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 582 10 3 5 6.0 CC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL149188 41384 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 582 10 3 5 6.0 CC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365595 42270 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 485 10 4 4 6.0 CNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL149992 42270 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 485 10 4 4 6.0 CNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44292785 176423 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL46268 176423 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44365865 193117 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 513 12 4 4 6.8 CCCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL538660 193117 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 513 12 4 4 6.8 CCCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44444670 94030 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 94030 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444678 154388 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 154388 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
44417614 141074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
9917213 201708 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 627 11 1 8 5.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL65569 201708 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 627 11 1 8 5.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11642933 77741 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210277 77741 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44412946 77746 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 656 11 2 7 8.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)Nc4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210295 77746 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 656 11 2 7 8.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)Nc4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
70697569 77605 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL2096778 77605 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365252 37551 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3csc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL145840 37551 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3csc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44322402 204470 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86490 204470 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44322443 204758 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 3 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL88293 204758 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 3 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
9873394 79494 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 596 12 0 8 7.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(CC)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212472 79494 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 596 12 0 8 7.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(CC)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11635837 138545 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccc(OC)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378654 138545 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccc(OC)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11527301 138686 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2cccc(F)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378845 138686 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2cccc(F)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44267057 8242 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 411 9 3 2 6.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10929 8242 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 411 9 3 2 6.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)c1 10.1016/s0960-894x(01)00134-2
44267073 9130 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 414 9 2 1 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(F)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11067 9130 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 414 9 2 1 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(F)cc2)c1 10.1016/s0960-894x(01)00134-2
44267029 9142 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 551 12 3 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11074 9142 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 551 12 3 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)c1 10.1016/s0960-894x(01)00134-2
44402105 124270 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL364246 124270 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
44391499 65587 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183600 65587 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365598 41387 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149189 41387 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365351 121476 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL359370 121476 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
15462666 96042 4 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96042 4 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44365028 42209 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 457 10 3 4 5.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC(=O)CCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149940 42209 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 457 10 3 4 5.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC(=O)CCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44214065 120541 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 534 14 2 4 7.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(OCc3ccccc3)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL356970 120541 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 534 14 2 4 7.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(OCc3ccccc3)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
162667361 181933 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 181933 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162675445 182816 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 182816 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL428186 211667 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N(C)CC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573586 186908 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494232 186908 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44346667 113231 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10930638 98559 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402466 71526 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197089 71526 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44573713 192277 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL522202 192277 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
44391754 168097 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436472 168097 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436874 211931 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL None None None None 10.1021/jm0506928
162650892 179639 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179639 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
9982147 204556 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL87020 204556 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44365644 41375 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 612 11 3 6 6.6 CCOC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL149181 41375 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 612 11 3 6 6.6 CCOC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365772 42127 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 539 10 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149881 42127 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 539 10 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44561397 189222 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189222 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44359301 11516 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180754 11516 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141221 11516 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44358957 12023 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184158 12023 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336039 12023 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293130 181300 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47791 181300 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293131 188242 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50663 188242 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44214072 176834 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 484 11 3 4 6.5 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL46385 176834 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 484 11 3 4 6.5 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
9982147 204556 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL87020 204556 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44406776 133806 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44573625 186938 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494415 186938 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44359303 11517 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180760 11517 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141539 11517 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44391714 121608 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL359668 121608 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44402571 124420 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL364297 124420 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391498 165556 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL426060 165556 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
67144370 174033 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4557575 174033 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143547 170940 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464132 170940 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11626096 186677 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
CHEMBL492780 186677 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
44444678 154388 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 154388 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
11620431 178779 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178779 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11671279 130349 0 None 331 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130349 0 None 331 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44402492 125650 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
CHEMBL364933 125650 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
44402471 134685 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL372316 134685 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391548 65687 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183698 65687 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44561105 186159 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 476 6 3 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL488812 186159 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 476 6 3 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44417615 141379 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 14354 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402572 70835 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 2 7 4.6 CNC(=O)Nc1ccc2c(c1)nc(SCc1cc([N+](=O)[O-])ccc1OC)n2C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195626 70835 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 2 7 4.6 CNC(=O)Nc1ccc2c(c1)nc(SCc1cc([N+](=O)[O-])ccc1OC)n2C(C)C 10.1016/j.bmcl.2005.03.030
44444647 154450 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 154450 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
44444676 154387 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 154387 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
118179235 181343 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4779806 181343 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
118179051 179628 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179628 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573110 186601 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 186601 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44577104 178159 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178159 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
11294792 62943 0 None 380 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62943 0 None 380 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
67143679 173579 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 544 8 1 6 4.8 Cc1c(N2CCC(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4546864 173579 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 544 8 1 6 4.8 Cc1c(N2CCC(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143755 174843 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4576169 174843 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44391826 64536 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
CHEMBL182178 64536 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
44444645 154449 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 154449 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
162665107 181544 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4782228 181544 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44444626 154332 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 154332 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
44402464 168512 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL439860 168512 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211931 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL None None None None 10.1021/jm0506928
67143749 169568 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 561 8 2 8 3.4 Cc1c(N2CCN(Cc3ccc(O)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4444237 169568 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 561 8 2 8 3.4 Cc1c(N2CCN(Cc3ccc(O)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143490 171033 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4465381 171033 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11525358 186749 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL493185 186749 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44417615 141379 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402360 132909 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 505 7 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1-c1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL370623 132909 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 505 7 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1-c1ccccc1 10.1016/j.bmcl.2005.03.030
67143710 169757 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447139 169757 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9979079 8264 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10931 8264 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
9979079 8264 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL10931 8264 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
162660654 180708 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4762368 180708 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44322400 204550 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL86976 204550 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCCN2)c1 10.1016/s0960-894x(99)00447-3
44322420 204958 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 5 2 6 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL89672 204958 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 5 2 6 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00447-3
44293274 100773 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 100773 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293594 101083 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 101083 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293134 186808 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186808 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44348278 156325 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2cccnc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407193 156325 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2cccnc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44267048 162657 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 475 10 3 3 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(S(N)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL418339 162657 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 475 10 3 3 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(S(N)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
44267256 9059 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 447 9 2 2 7.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cnc3ccccc3c2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11014 9059 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 447 9 2 2 7.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cnc3ccccc3c2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL2430900 208706 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
67143674 174487 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4568223 174487 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402105 124270 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL364246 124270 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
44346397 113987 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162645007 178871 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573625 186938 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494415 186938 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
15602806 8197 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8197 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44402553 71074 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196079 71074 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL None None None None 10.1021/jm0506928
CHEMBL330173 209574 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
10919052 113007 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44444668 153733 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 153733 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143804 172615 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4522657 172615 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179169 179336 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4746174 179336 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44328354 96694 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 980 24 9 10 0.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL267986 96694 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 980 24 9 10 0.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11518185 187095 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495190 187095 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
10930638 98559 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391734 122090 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360297 122090 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 133806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
10919052 113007 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141074 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 113007 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391692 63954 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181057 63954 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
25194091 188413 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 188413 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44322502 205237 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 390 4 1 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(C)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL91311 205237 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 390 4 1 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(C)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44309572 202626 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
CHEMBL71561 202626 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
44352512 116783 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
CHEMBL339636 116783 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
10484172 98571 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 632 12 3 6 5.8 CCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL280296 98571 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 632 12 3 6 5.8 CCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL None None None None 10.1021/jm0506928
10649568 14382 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of binding to GnRH receptor in ratIn vitro inhibition of binding to GnRH receptor in rat
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of binding to GnRH receptor in ratIn vitro inhibition of binding to GnRH receptor in rat
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
10649568 14382 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of Rat gonadotropin-releasing hormone receptorInhibition of Rat gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
CHEMBL120432 14382 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of Rat gonadotropin-releasing hormone receptorInhibition of Rat gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
9936667 100039 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL291201 100039 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293071 101117 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 101117 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293208 170567 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL445848 170567 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292988 181849 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 181849 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
1184 3663 31 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3663 31 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3663 31 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
10603202 168026 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL435974 168026 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
1184 3663 31 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 3663 31 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 3663 31 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL3085508 209233 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL None None None None 10.1021/jm0506928
67142818 173465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4543788 173465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11478448 65730 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183779 65730 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
1185 3632 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
15602804 7983 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7983 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44321496 105470 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL312995 105470 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211931 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44341080 110076 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL325417 110076 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL436874 211931 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL None None None None 10.1021/jm0506928
44321291 204544 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86950 204544 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321292 204553 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87000 204553 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211931 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL None None None None 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44293804 101316 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300095 101316 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44593424 175549 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175549 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL436874 211931 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL None None None None 10.1021/jm0506928
44593424 175549 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175549 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
71623059 180233 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180233 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44365898 119138 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 442 10 3 3 6.3 COc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL346903 119138 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 442 10 3 3 6.3 COc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44593424 175549 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175549 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44593424 175549 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175549 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44346397 113987 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
9961721 167903 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9961721 167903 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44358962 12022 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184155 12022 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL335764 12022 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44267238 96059 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL262715 96059 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44413009 79340 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 537 9 1 7 6.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211808 79340 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 537 9 1 7 6.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44266961 9054 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 518 13 4 3 5.9 CCNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11011 9054 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 518 13 4 3 5.9 CCNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267238 96059 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL262715 96059 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44365269 39613 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1ccc(C)c(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL147740 39613 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1ccc(C)c(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44274327 81757 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 589 10 0 7 6.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(CC(C)C)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21704 81757 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 589 10 0 7 6.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(CC(C)C)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
15462660 82400 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 623 10 0 7 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(Cc2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21804 82400 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 623 10 0 7 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(Cc2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
10930638 98559 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10930638 98559 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346397 113987 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
11527384 77122 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2cccc(OC)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL208714 77122 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2cccc(OC)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11226884 77300 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccc(F)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL208904 77300 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccc(F)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
71459964 79072 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 573 10 2 5 7.7 Cc1cc(C)cc(-c2c(OCC[C@@H]3CCC[C@H](CCCc4ccccc4)N3)c3cc([N+](=O)[O-])c(Cl)cc3[nH]c2=O)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2113713 79072 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 573 10 2 5 7.7 Cc1cc(C)cc(-c2c(OCC[C@@H]3CCC[C@H](CCCc4ccccc4)N3)c3cc([N+](=O)[O-])c(Cl)cc3[nH]c2=O)c1 10.1016/j.bmcl.2003.12.101
44391784 121799 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL359860 121799 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365171 38579 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 416 9 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL146678 38579 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 416 9 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44417614 141074 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 113007 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322380 204791 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.0 CN1CCCC(COc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
CHEMBL88516 204791 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.0 CN1CCCC(COc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
44322302 204920 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89332 204920 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44391510 122411 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360693 122411 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
67143420 162346 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4173938 162346 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
145948911 166912 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1304 29 16 15 -1.1 NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1 10.1039/C5MD00259A
CHEMBL4299453 166912 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1304 29 16 15 -1.1 NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1 10.1039/C5MD00259A
86275342 115673 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
CHEMBL3358413 115673 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
118179051 179628 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179628 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
11634198 186773 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 186773 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44267278 9205 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 3 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11101 9205 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 3 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)nc2)c1 10.1016/s0960-894x(01)00133-0
44402645 168547 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL440212 168547 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL None None None None 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44402646 132900 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370587 132900 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
87285550 173746 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4550720 173746 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71668147 179400 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4746969 179400 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67143723 174816 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 8 3.8 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4575491 174816 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 8 3.8 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL406243 210843 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NC1(C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)CCC1 10.1021/jm990433g
44402463 126989 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL366236 126989 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL None None None None 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
118178986 181607 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
CHEMBL4782882 181607 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
11167850 2691 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
86272223 115675 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
CHEMBL3358415 115675 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
11525358 186749 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL493185 186749 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44444675 154172 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 154172 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44402293 71069 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
CHEMBL196040 71069 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
86275345 181478 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 181478 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
15602808 8010 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8010 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44417615 141379 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113231 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
162649425 179430 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4747322 179430 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL327359 209535 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44359224 11509 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
CHEMBL1180706 11509 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
CHEMBL138977 11509 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
44293165 101210 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 101210 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44267275 97674 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 490 11 3 4 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL273625 97674 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 490 11 3 4 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)nc2)c1 10.1016/s0960-894x(01)00133-0
44295820 101502 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCCC2C)c1 10.1016/j.bmcl.2003.12.101
CHEMBL301501 101502 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCCC2C)c1 10.1016/j.bmcl.2003.12.101
44402467 170079 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL445143 170079 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL410269 211053 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11518185 187095 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495190 187095 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44346397 113987 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44267254 9174 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11087 9174 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
44267271 9699 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 386 9 3 2 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2c[nH]cn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11375 9699 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 386 9 3 2 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2c[nH]cn2)c1 10.1016/s0960-894x(01)00133-0
11318649 64008 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181257 64008 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44561142 186111 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4ccc5[nH]c(=S)[nH]c5c4)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL488478 186111 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4ccc5[nH]c(=S)[nH]c5c4)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44346397 113987 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44267242 9942 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11523 9942 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44573791 186795 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 186795 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
145950097 162240 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 8 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172391 162240 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 8 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
118178976 180589 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4761024 180589 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573789 186747 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493167 186747 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
15602807 8121 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8121 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44572236 171323 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171323 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44267035 96750 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 504 12 4 3 5.5 CNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL268479 96750 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 504 12 4 3 5.5 CNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44402499 69465 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
CHEMBL193689 69465 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
44406776 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3632 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44391499 65587 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183600 65587 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
162647697 179269 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4745391 179269 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
53239184 169023 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436375 169023 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267054 9687 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 468 10 4 2 6.4 CNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11368 9687 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 468 10 4 2 6.4 CNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
67144478 169772 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccc(F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4447332 169772 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccc(F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44406776 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL None None None None 10.1021/jm0506928
90663998 106333 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 787 14 4 10 4.9 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](CC1=CNCN1)NC(=O)[C@@H]1CCCN1C(=O)OCC(c1ccccc1)c1ccccc1 10.1021/jm00129a003
CHEMBL3144569 106333 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 787 14 4 10 4.9 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](CC1=CNCN1)NC(=O)[C@@H]1CCCN1C(=O)OCC(c1ccccc1)c1ccccc1 10.1021/jm00129a003
44417615 141379 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44387961 165457 0 None 144 2 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165457 0 None 144 2 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44391510 122411 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360693 122411 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
162667361 181933 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 181933 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162645007 178871 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573791 186795 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 186795 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44573276 186823 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 186823 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
11226753 62999 0 None 389 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 62999 0 None 389 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
44406776 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
87285708 173323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4540232 173323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145957335 161743 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 519 7 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)C3CCSCC3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4164417 161743 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 519 7 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)C3CCSCC3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44402646 132900 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370587 132900 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
44391628 65526 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183572 65526 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391754 168097 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436472 168097 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
53239184 169023 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436375 169023 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444641 154418 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 154418 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143715 172906 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4530350 172906 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44305604 201715 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 625 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C4CC4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL65614 201715 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 625 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C4CC4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11282957 121806 0 None 1096 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121806 0 None 1096 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
44292919 100663 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100663 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293305 100978 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 100978 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44292990 100715 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL295731 100715 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293178 100939 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 100939 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292979 187596 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49893 187596 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44348173 169903 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 39 15 17 1.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL444903 169903 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 39 15 17 1.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
67143432 171551 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4472942 171551 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
11526254 187020 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 504 5 1 7 4.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccnc(S(C)(=O)=O)n5)CC4)cccc3[nH]2)cc1 10.1021/jm701249f
CHEMBL494797 187020 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 504 5 1 7 4.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccnc(S(C)(=O)=O)n5)CC4)cccc3[nH]2)cc1 10.1021/jm701249f
CHEMBL3085508 209233 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44321695 105488 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313086 105488 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209233 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44348310 157267 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
CHEMBL408335 157267 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
155531714 175607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
44406776 133806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL None None None None 10.1021/jm0506928
145952094 162343 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 523 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(C)cc3C)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4173914 162343 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 523 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(C)cc3C)c2=O)c1F 10.1016/j.ejmech.2017.12.095
86275573 115676 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
CHEMBL3358416 115676 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
44561397 189222 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189222 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11167850 2691 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44348418 96184 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263629 96184 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44321510 106642 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316159 106642 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211931 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL None None None None 10.1021/jm0506928
44572236 171323 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171323 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44561369 189864 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189864 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL436874 211931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL None None None None 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
15602805 8008 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8008 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44292888 174196 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45614 174196 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44295630 190224 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 8 3 7 6.6 CCC1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL51841 190224 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 8 3 7 6.6 CCC1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL436874 211931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL None None None None 10.1021/jm0506928
24825725 192017 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192017 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL436874 211931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL None None None None 10.1021/jm0506928
9979079 8264 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL10931 8264 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462657 79798 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 609 9 0 7 6.8 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21373 79798 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 609 9 0 7 6.8 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9979079 8264 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL10931 8264 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
25193798 169620 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 169620 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
9961721 167903 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9979079 8264 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL10931 8264 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44267231 9490 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11253 9490 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44391735 121810 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL359914 121810 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL436874 211931 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44365420 40964 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccccc1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL148884 40964 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccccc1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
90663997 106332 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 849 14 6 11 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNCN1)C(=O)NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1 10.1021/jm00129a003
CHEMBL3144568 106332 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 849 14 6 11 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNCN1)C(=O)NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1 10.1021/jm00129a003
44417614 141074 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 113007 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322401 106055 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 2 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL314147 106055 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 2 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00446-1
44322444 204896 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 1 4 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89186 204896 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 1 4 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
11570616 77888 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 506 9 0 8 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)C)c2c1=O 10.1021/jm0512894
CHEMBL210845 77888 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 506 9 0 8 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)C)c2c1=O 10.1021/jm0512894
44412978 79333 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211752 79333 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44267086 97613 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 441 10 2 3 6.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL273296 97613 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 441 10 2 3 6.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)c1 10.1016/s0960-894x(01)00134-2
10603202 168026 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL435974 168026 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
44365118 41293 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 473 12 2 5 5.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149124 41293 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 473 12 2 5 5.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)cc1OC 10.1016/s0960-894x(00)00707-1
11167850 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44346398 14354 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 141379 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
11511860 138791 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 476 8 0 7 5.1 CCOC(=O)c1cn(C)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379274 138791 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 476 8 0 7 5.1 CCOC(=O)c1cn(C)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11167850 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44573113 192625 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL523711 192625 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44444665 93754 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 93754 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444652 94053 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 94053 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402466 71526 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197089 71526 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44391693 63421 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL180167 63421 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67144162 174471 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 657 9 1 8 4.3 Cc1c(N2CCN(Cc3cccc([S+](C)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567854 174471 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 657 9 1 8 4.3 Cc1c(N2CCN(Cc3cccc([S+](C)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402403 71170 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196288 71170 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
44561141 192887 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 192887 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44346397 113987 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113231 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113231 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL436874 211931 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL None None None None 10.1021/jm0506928
87285768 169917 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169917 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
25193700 172701 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 172701 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11167850 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44417615 141379 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
87285521 174437 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567165 174437 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444644 154448 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401350 154448 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143487 170186 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 662 9 1 9 5.2 Cc1c(N2CCN(Cc3cccc(-c4ncco4)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4452636 170186 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 662 9 1 9 5.2 Cc1c(N2CCN(Cc3cccc(-c4ncco4)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
123549935 178844 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4740379 178844 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
162672599 182415 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4793643 182415 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
44391703 167927 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL435334 167927 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
162665107 181544 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4782228 181544 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
10919052 113007 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391526 122078 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360244 122078 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
86275342 115673 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL3358413 115673 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44402465 134699 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL372455 134699 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
44391821 65235 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183197 65235 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67143432 171551 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4472942 171551 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
127037454 136927 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1250 31 17 15 -2.5 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3753755 136927 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1250 31 17 15 -2.5 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
9918188 154171 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 154171 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44444649 154454 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 154454 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44293164 167257 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL430763 167257 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44402670 71599 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197317 71599 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL318127 209455 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCCN)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573626 186939 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494416 186939 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
118179174 181884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4786609 181884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
87285732 172373 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4517137 172373 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118178989 180562 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4760799 180562 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44444635 154154 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 154154 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402472 132287 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370145 132287 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44406776 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
162645007 178871 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573278 186854 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL493932 186854 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44573277 186853 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493931 186853 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44267239 96650 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 413 9 3 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL267558 96650 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 413 9 3 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00133-0
44293285 162213 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL417189 162213 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402057 71579 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL197254 71579 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391693 63421 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL180167 63421 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 133806 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
162645007 178871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44402672 71276 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 420 7 1 6 5.1 COc1ccc(C#N)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196351 71276 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 420 7 1 6 5.1 COc1ccc(C#N)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44573112 187005 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494739 187005 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
11583388 8191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092626 8191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44346397 113987 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162650892 179639 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179639 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44561141 192887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 192887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44391498 165556 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL426060 165556 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
118179127 182622 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
CHEMBL4795998 182622 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
127036617 137004 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1236 31 17 15 -2.9 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3754384 137004 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1236 31 17 15 -2.9 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
155531714 175607 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175607 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
44365609 39451 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 11 3 6 5.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(C)(=O)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL147537 39451 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 11 3 6 5.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(C)(=O)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
10930638 98559 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44406776 133806 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293366 161650 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 161650 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293236 174297 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL45639 174297 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
10674894 25321 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL135103 25321 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL438652 212027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
10674894 25321 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL135103 25321 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
11980076 206701 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 206701 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
44321497 97629 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL273390 97629 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL None None None None 10.1021/jm0506928
11496945 175891 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175891 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
145957893 161509 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 545 8 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cc(F)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4160683 161509 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 545 8 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cc(F)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11455317 62544 0 None 851 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62544 0 None 851 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
1185 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44402396 161118 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL413216 161118 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402397 161306 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL414899 161306 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
87285768 169917 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169917 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402397 161306 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL414899 161306 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL3085508 209233 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL None None None None 10.1021/jm0506928
11180219 110720 0 None 112 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110720 0 None 112 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
67142995 169748 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccoc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446997 169748 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccoc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44577104 178159 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1021/jm701249f
CHEMBL468565 178159 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1021/jm701249f
11167850 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL None None None None 10.1021/jm0506928
11532637 7618 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7618 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44406776 133806 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144450 171733 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4475210 171733 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402396 161118 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL413216 161118 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
67143570 171181 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467407 171181 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71623059 180233 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180233 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
1184 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
9874838 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
CHEMBL71917 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
1184 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9874838 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
CHEMBL71917 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9961721 167903 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9961721 167903 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10649568 14382 0 None 10 2 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of binding to gonadotropin-releasing hormone receptor in dogIn vitro inhibition of binding to gonadotropin-releasing hormone receptor in dog
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14382 0 None 10 2 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of binding to gonadotropin-releasing hormone receptor in dogIn vitro inhibition of binding to gonadotropin-releasing hormone receptor in dog
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
1184 3663 31 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
9874838 3663 31 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
CHEMBL71917 3663 31 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
1184 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
9874838 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
CHEMBL71917 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
1184 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
1184 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
1184 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 3663 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
44406776 133806 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211931 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL None None None None 10.1021/jm0506928
44365078 41198 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 414 10 3 3 5.7 COc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL149062 41198 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 414 10 3 3 5.7 COc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365456 42533 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 11 3 2 7.1 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL150223 42533 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 11 3 2 7.1 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462666 96042 4 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96042 4 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141074 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44292915 182299 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 590 12 3 4 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)O)cc3c2CCN(CCCCc2ccc(O)cc2)C(=O)OCc2ccccc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47921 182299 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 590 12 3 4 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)O)cc3c2CCN(CCCCc2ccc(O)cc2)C(=O)OCc2ccccc2)c1 10.1016/s0960-894x(01)00274-8
44402378 69318 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL193529 69318 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391612 63153 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL179977 63153 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365170 40196 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 430 10 3 4 5.3 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148245 40196 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 430 10 3 4 5.3 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44417614 141074 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67144531 172572 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(C#N)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4521484 172572 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(C#N)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162670223 181979 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4787856 181979 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44573790 192649 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
CHEMBL523849 192649 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
44402464 168512 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL439860 168512 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
44402404 133028 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL371073 133028 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
87285668 173137 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 669 8 1 8 5.6 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4536130 173137 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 669 8 1 8 5.6 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444672 168825 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 168825 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44402538 167860 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL434955 167860 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402538 167860 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL434955 167860 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
145954593 161971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(F)cc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167945 161971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(F)cc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133806 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44296134 187804 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCC(C)CN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL50182 187804 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCC(C)CN2)c1 10.1016/j.bmcl.2003.12.101
44406776 133806 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44402232 71052 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195920 71052 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44561265 172528 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452044 172528 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44322336 105647 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 398 6 1 4 5.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC(C)CN(C)C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL313517 105647 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 398 6 1 4 5.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC(C)CN(C)C)c1 10.1016/s0960-894x(99)00446-1
44402462 69547 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 399 6 1 4 5.9 CC(C)n1c(SCc2ccccc2Cl)nc2cc(NC(=O)C3CC3)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193897 69547 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 399 6 1 4 5.9 CC(C)n1c(SCc2ccccc2Cl)nc2cc(NC(=O)C3CC3)ccc21 10.1016/j.bmcl.2005.03.030
67144164 173304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
CHEMBL4539811 173304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
44215908 93781 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 93781 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444630 154273 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 154273 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44561108 185838 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 185838 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
71666542 179757 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4751345 179757 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL436874 211931 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL None None None None 10.1021/jm0506928
67143743 170729 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cc1 10.1021/acs.jmedchem.6b01071
CHEMBL4460966 170729 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cc1 10.1021/acs.jmedchem.6b01071
67144486 170663 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3C(F)(F)F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4459812 170663 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3C(F)(F)F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143407 170191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4452793 170191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402377 132905 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1cccc(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
CHEMBL370603 132905 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1cccc(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
44391703 167927 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL435334 167927 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL436874 211931 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL None None None None 10.1021/jm0506928
162645007 178871 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44402293 71069 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
CHEMBL196040 71069 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
44391526 122078 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360244 122078 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
86272223 115675 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
CHEMBL3358415 115675 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
118179235 181343 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4779806 181343 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573714 187093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 2 4 5.2 Cc1n[nH]c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495189 187093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 2 4 5.2 Cc1n[nH]c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44561368 176230 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176230 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44573275 186822 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493730 186822 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
44402465 134699 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL372455 134699 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
145949379 162152 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 496 7 1 7 3.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccnc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4170863 162152 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 496 7 1 7 3.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccnc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL3085508 209233 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44391734 122090 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360297 122090 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44391692 63954 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181057 63954 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44444644 154448 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401350 154448 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44365844 41671 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 12 3 6 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(=O)(=O)C(C)C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149447 41671 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 12 3 6 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(=O)(=O)C(C)C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL97265 214136 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
24825725 192017 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 192017 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44305274 102283 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 667 11 1 9 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccsc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL305155 102283 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 667 11 1 9 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccsc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
44293222 175377 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 175377 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 175377 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11525358 186749 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmc.2012.09.013
CHEMBL493185 186749 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmc.2012.09.013
10074296 9283 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL11149 9283 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL438652 212027 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
10074296 9283 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11149 9283 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
10074296 9283 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11149 9283 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
10074296 9283 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
CHEMBL11149 9283 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
11980076 206701 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 206701 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
67144646 172556 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3cocn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4521118 172556 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3cocn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155559612 174301 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1612 43 20 24 -4.1 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CCCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4563936 174301 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1612 43 20 24 -4.1 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CCCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
44292918 170839 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170839 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
67143413 169039 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4436711 169039 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 209233 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
70691201 77285 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
CHEMBL2088506 77285 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
11604354 186931 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 186931 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
11167850 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
145952802 162035 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 579 8 1 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccc(OC(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4169027 162035 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 579 8 1 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccc(OC(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL3085508 209233 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL94842 214125 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44417614 141074 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141074 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10722009 116040 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL336319 116040 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44295982 187706 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2Cc3ccccc3CN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL50035 187706 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2Cc3ccccc3CN2)c1 10.1016/j.bmcl.2003.12.101
10722009 116040 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL336319 116040 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
44365281 42537 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1cc(OC)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL150228 42537 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1cc(OC)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462665 168083 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 615 9 0 7 7.4 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(C2CCCCC2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL436346 168083 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 615 9 0 7 7.4 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(C2CCCCC2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44412876 77542 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccccc3OC)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL209419 77542 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccccc3OC)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10985312 78321 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78321 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44322390 204874 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 3 1 4 5.1 CN1CCCCC(Oc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
CHEMBL89041 204874 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 3 1 4 5.1 CN1CCCCC(Oc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
11512807 139593 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 610 11 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(Cc3ccccc3)C(C)=O)c2c1=O 10.1021/jm0512894
CHEMBL380200 139593 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 610 11 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(Cc3ccccc3)C(C)=O)c2c1=O 10.1021/jm0512894
44573507 186961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 4 5.8 Cc1ccc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494548 186961 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 4 5.8 Cc1ccc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
11496610 4000 11 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4000 11 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4000 11 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
25193798 169620 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 169620 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10919052 113007 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402038 69849 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL194074 69849 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44346398 14354 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14354 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162675445 182816 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 182816 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL2370256 208065 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44561369 189864 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189864 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11496610 4000 11 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4000 11 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4000 11 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44391613 167701 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
CHEMBL433954 167701 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
127036774 136971 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1146 25 12 13 -1.5 CC(C)C[C@H](NC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@@H]3CCC(=O)N3)CC2)C1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3754120 136971 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1146 25 12 13 -1.5 CC(C)C[C@H](NC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@@H]3CCC(=O)N3)CC2)C1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
162645007 178871 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
145949556 162371 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4174298 162371 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
67142794 173541 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4545859 173541 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
162645007 178871 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178871 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL428619 211703 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444649 154454 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 154454 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44185958 154447 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 154447 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44573586 186908 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494232 186908 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44391821 65235 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183197 65235 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67143567 170693 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCC(C)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4460413 170693 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCC(C)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44295833 167336 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCc3ccccc32)c1 10.1016/j.bmcl.2003.12.101
CHEMBL431344 167336 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCc3ccccc32)c1 10.1016/j.bmcl.2003.12.101
11318649 64008 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181257 64008 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44322434 110915 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 6 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCCN2CCCCC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL327323 110915 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 6 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCCN2CCCCC2)c1 10.1016/s0960-894x(99)00446-1
44444673 93834 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 93834 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
118179169 179336 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4746174 179336 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
162656174 180282 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4757424 180282 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44573111 187004 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494738 187004 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44444628 93870 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 93870 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402616 70777 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
CHEMBL195516 70777 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
44391718 65259 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183325 65259 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44593415 188780 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188780 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44573276 186823 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 186823 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
11167850 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44444626 154332 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 154332 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
11592658 79326 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 642 11 2 6 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)NC(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211731 79326 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 642 11 2 6 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)NC(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL436874 211931 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL None None None None 10.1021/jm0506928
44341186 9934 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL115192 9934 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL436874 211931 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL None None None None 10.1021/jm0506928
44293378 101410 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300792 101410 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
1185 3632 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44561368 176230 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176230 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44406776 133806 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144496 169256 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439817 169256 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44274248 98207 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2Cl)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277435 98207 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2Cl)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
11167850 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67143514 172819 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCCC(C)C2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4528231 172819 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCCC(C)C2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44593415 188780 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1021/jm701249f
CHEMBL512893 188780 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1021/jm701249f
10930638 98559 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98559 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 141379 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141379 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10674894 25321 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL135103 25321 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL261927 208766 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
15602807 8121 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8121 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44391628 65526 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183572 65526 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44406776 133806 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44391542 64881 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182639 64881 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44573753 186878 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494021 186878 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44391735 121810 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL359914 121810 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
44391771 165458 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL425524 165458 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
86275343 182899 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4799511 182899 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44391835 165740 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL427146 165740 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15895696 111959 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL329834 111959 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44573585 186647 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL492587 186647 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
67143612 170473 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456937 170473 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44359289 12030 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184180 12030 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL337323 12030 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44402616 70777 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
CHEMBL195516 70777 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
11167850 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1178 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1187 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL179691 2691 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
118179135 181426 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 181426 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44572286 180209 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180209 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44406776 133806 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2370262 208068 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccccn1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444675 154172 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 154172 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44402038 69849 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL194074 69849 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402673 132734 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL370414 132734 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391670 64346 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
CHEMBL181864 64346 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
67143618 169716 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446435 169716 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143023 174415 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4566719 174415 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155531714 175607 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175607 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
145949399 162172 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 8 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(C(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4171288 162172 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 8 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(C(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
9961721 167903 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167903 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359254 11512 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL1180716 11512 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL139292 11512 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
11549071 138404 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 11 2 7 6.4 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CN)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378481 138404 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 11 2 7 6.4 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CN)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10985312 78321 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78321 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
70691201 77285 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
CHEMBL2088506 77285 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
11167850 2691 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44348333 96432 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL265727 96432 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL3085508 209233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3632 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
15602806 8197 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8197 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
71623059 180233 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180233 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
118179135 181426 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 181426 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44573585 186647 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL492587 186647 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44267240 9589 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 427 10 2 3 6.0 COc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
CHEMBL11310 9589 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 427 10 2 3 6.0 COc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
44365088 120968 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 10 3 2 6.3 CCc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL358260 120968 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 10 3 2 6.3 CCc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365500 164720 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1C 10.1016/s0960-894x(00)00707-1
CHEMBL423215 164720 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1C 10.1016/s0960-894x(00)00707-1
44417614 141074 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141074 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346397 113987 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 113987 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44365374 41399 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL149196 41399 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1 10.1016/s0960-894x(00)00707-1
44365249 120550 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 370 6 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL357025 120550 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 370 6 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44322272 204448 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.1 CN1CCCCC1COc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
CHEMBL86365 204448 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.1 CN1CCCCC1COc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
44322052 204959 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 356 6 1 4 4.6 CN(C)CCCOc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
CHEMBL89675 204959 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 356 6 1 4 4.6 CN(C)CCCOc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
44267257 9258 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11134 9258 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
118178989 180562 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4760799 180562 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
71666685 182122 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4789613 182122 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67144496 169256 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439817 169256 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
86275573 115676 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
CHEMBL3358416 115676 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
44444663 93753 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 93753 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
1185 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3632 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44391525 165802 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL427500 165802 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
15602804 7983 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7983 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
10919052 113007 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113007 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44561108 185838 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 185838 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL436874 211931 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL None None None None 10.1021/jm0506928
44444630 154273 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 154273 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44391542 64881 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182639 64881 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11626096 186677 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
CHEMBL492780 186677 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
11167850 2691 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2691 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2691 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2691 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44402648 70938 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 453 8 1 7 5.1 COC(=O)c1ccc(OC)c(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
CHEMBL195726 70938 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 453 8 1 7 5.1 COC(=O)c1ccc(OC)c(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
118167818 178842 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 178842 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
118179051 179628 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179628 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
25193797 189063 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 189063 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL414113 211352 0 None - 1 Rat 10.1 pKd = 10.1 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
101609491 141272 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
44317046 141272 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
77058850 141272 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
CHEMBL386314 141272 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
1190 867 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
25074887 867 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
583 867 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
CHEMBL1200490 867 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
DB00050 867 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
CHEMBL2369860 207957 0 None - 1 Rat 9.7 pKd = 9.7 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370807 208168 0 None - 1 Human 9.7 pKd = 9.7 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
3823 49936 38 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49936 38 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49936 38 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL414391 211372 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None C/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](CCCCN/C(=N\C)NC#N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL407225 210892 0 None - 1 Rat 9.6 pKd = 9.6 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O)c1cccnc1)c1cccnc1 10.1021/jm00398a030
CHEMBL266716 208939 0 None - 1 Human 9.6 pKd = 9.6 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL218396 207640 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL269583 209043 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CCCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL376017 210483 0 None - 1 Rat 9.6 pKd = 9.6 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@H]1C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)O 10.1021/jm00398a030
CHEMBL438762 212037 0 None - 1 Rat 9.5 pKd = 9.5 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(/NC#N)NC(C)C)NC(=O)[C@H](CCCC/N=C(/NC#N)NC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370809 208170 0 None - 1 Human 9.5 pKd = 9.5 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNC(=O)c1cccnc1)C(=O)N[C@@H](CCCCNC(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
10348973 3249 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5432 3249 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5586 3249 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL1800159 3249 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
DB11853 3249 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
3823 49936 38 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49936 38 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49936 38 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL261999 208770 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
44316759 168291 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1537 45 17 19 -0.7 CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL438191 168291 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1537 45 17 19 -0.7 CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2369851 207956 0 None - 1 Rat 9.3 pKd = 9.3 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370818 208172 0 None - 1 Human 9.3 pKd = 9.3 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL441741 212135 0 None - 1 Rat 9.2 pKd = 9.2 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00398a030
CHEMBL2370808 208169 0 None - 1 Human 9.2 pKd = 9.2 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL439892 212094 0 None - 1 Rat 9.1 pKd = 9.1 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
10348973 3249 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5432 3249 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5586 3249 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL1800159 3249 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
DB11853 3249 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL2370803 208167 0 None - 1 Human 9.1 pKd = 9.1 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm00101a003
CHEMBL2370814 208171 0 None - 1 Human 9.1 pKd = 9.1 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CCNC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm00101a003
CHEMBL407482 210907 0 None - 1 Rat 9.0 pKd = 9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL411806 211202 0 None - 1 Rat 9.0 pKd = 9 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)NC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(C)=O)c1cccnc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(N)=O)c1cccnc1 10.1021/jm00398a030
CHEMBL436334 211921 0 None - 1 Rat 9.0 pKd = 9 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CCC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL2371272 208273 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CCC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL414149 211356 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
11250647 1510 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
5293 1510 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
8362 1510 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL1208155 1510 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
DB11979 1510 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL407023 210875 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL439359 212081 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(\NC#N)NC1CCCCC1)NC(=O)[C@H](CCCC/N=C(\NC#N)NC1CCCCC1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL411586 211189 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCCN/C(=N/CCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL412802 211269 0 None - 1 Rat 8.8 pKd = 8.8 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2371274 208275 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL2371275 208276 0 None - 1 Rat 8.0 pKd = 8 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL442303 212151 0 None - 1 Rat 8.0 pKd = 8 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL265825 208910 0 None - 1 Rat 8.0 pKd = 8.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL428837 211721 0 None - 1 Rat 8.7 pKd = 8.7 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCN/C(=N/CCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
11250647 1510 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
5293 1510 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
8362 1510 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL1208155 1510 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
DB11979 1510 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL265522 208897 0 None - 1 Rat 8.5 pKd = 8.5 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCCN/C(=N/CCCCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL442303 212151 0 None - 1 Rat 8.4 pKd = 8.4 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL2371273 208274 0 None - 1 Rat 7.4 pKd = 7.4 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
12784 571 8 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL2371277 208278 0 None - 1 Rat 8.2 pKd = 8.2 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
3823 49936 38 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49936 38 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49936 38 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
12784 571 8 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL409219 210997 0 None - 1 Rat 10.9 pKi = 10.9 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL268397 208996 0 None - 1 Rat 10.6 pKi = 10.6 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
44383749 96207 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1534 41 13 18 3.1 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC(N)C(=O)c1ccncc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL263839 96207 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1534 41 13 18 3.1 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC(N)C(=O)c1ccncc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL263840 208836 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL268319 208990 0 None - 1 Rat 10.3 pKi = 10.3 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None COc1ccc(C(=O)CC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm00059a020
44383968 158764 0 None - 1 Rat 10.2 pKi = 10.2 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1590 45 14 20 2.5 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL409990 158764 0 None - 1 Rat 10.2 pKi = 10.2 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1590 45 14 20 2.5 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL2371478 208296 0 None - 1 Rat 10.0 pKi = 10 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3c[nH]cn3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267907 16140 0 None 3 3 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 16140 0 None 3 3 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL438829 212043 0 None - 1 Rat 9.9 pKi = 9.9 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL2371592 208347 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990116+
CHEMBL386166 210620 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL405548 210808 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990118u
CHEMBL2371557 208328 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44379996 96379 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
91931282 96379 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL265240 96379 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44378966 95984 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL262160 95984 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL2371516 208312 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371582 208340 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371533 208319 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
11364940 177940 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 555 8 1 8 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466731 177940 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 555 8 1 8 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
1185 3632 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
3038517 3632 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
CHEMBL22055 3632 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
DB06494 3632 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
1184 3663 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
9874838 3663 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL71917 3663 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL2371483 208298 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371485 208300 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](CCCN=C(N)N)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371515 208311 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CN(C)C(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
23656390 161122 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 161122 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
1184 3663 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 3663 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 3663 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL407361 210900 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)N[C@H](C)C(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL439083 212061 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371514 208310 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371522 208316 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccc(Cl)cc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267812 97639 0 None 7 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 97639 0 None 7 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL438897 212046 0 None -1 2 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL438897 212046 0 None 1 2 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990118u
CHEMBL436657 211926 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL406809 210863 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371591 208346 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@H]1C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm990116+
CHEMBL269726 209049 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm990118u
CHEMBL2371507 208307 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44379287 160857 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1299 26 14 15 -1.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL412681 160857 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1299 26 14 15 -1.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44449120 94776 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94776 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44432648 149682 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 149682 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL411964 211208 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371537 208320 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CC[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
CHEMBL2371587 208344 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990116+
CHEMBL441208 212128 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990118u
CHEMBL2371566 208333 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CCNC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44378889 168580 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1251 27 13 16 -2.8 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H]1CC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL440436 168580 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1251 27 13 16 -2.8 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H]1CC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL2371519 208315 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267907 16140 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL12282 16140 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267907 16140 0 None -3 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 16140 0 None -3 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL2371568 208334 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371578 208337 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371517 208313 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CNC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44448991 154790 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154790 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154790 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL2371470 208295 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL2371486 208301 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CCNC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL410779 211082 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
9872676 77811 0 None 1 17 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant GnRH receptorBinding affinity to human recombinant GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77811 0 None 1 17 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant GnRH receptorBinding affinity to human recombinant GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
9872676 77811 0 None -1 17 Rat 9.4 pKi = 9.4 Binding
Binding affinity to rat pituitary GnRH receptorBinding affinity to rat pituitary GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77811 0 None -1 17 Rat 9.4 pKi = 9.4 Binding
Binding affinity to rat pituitary GnRH receptorBinding affinity to rat pituitary GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
10649568 14382 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
CHEMBL120432 14382 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
9961721 167903 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL435167 167903 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44432647 86299 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231954 86299 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL216634 207580 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11376252 69013 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
CHEMBL192955 69013 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
11376252 69013 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL192955 69013 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL2371577 208336 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL429007 211734 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11421412 178154 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL468551 178154 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44388510 165676 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 538 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1F 10.1021/jm049218c
CHEMBL426780 165676 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 538 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1F 10.1021/jm049218c
11421412 178154 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 178154 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432651 86262 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 86262 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432643 146222 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 146222 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11167850 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1178 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1187 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL179691 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
11167850 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
11167850 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
1178 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
1187 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
CHEMBL179691 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
11167850 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
1178 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
1187 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
CHEMBL179691 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
11167850 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 2691 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL2371579 208338 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@@H](C)NC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
CHEMBL2371508 208308 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](CCCN=C(N)N)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
11443711 10022 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL115703 10022 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
44346397 113987 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333518 113987 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44432652 96680 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 96680 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432654 159236 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 159236 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44400235 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
CHEMBL434936 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
10345138 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
44449681 95586 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL259906 95586 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
9854500 101789 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
CHEMBL303274 101789 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
9854500 101789 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
CHEMBL303274 101789 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
44400235 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL434936 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44400235 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL434936 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44400235 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL434936 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44400235 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL434936 167856 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
9854500 101789 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 101789 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44267887 98016 0 None -5 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 98016 0 None -5 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
10345138 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
CHEMBL360143 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
CHEMBL75347 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
44448991 154790 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154790 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154790 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
10345138 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL360143 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL75347 122029 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL2371541 208323 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CNC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44432653 86263 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 86263 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451355 157609 0 None - 1 Human 9.2 pKi = 9.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 577 11 2 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(C)CNCCCCc2ccnnc2)c1 10.1016/j.bmc.2007.09.026
CHEMBL408746 157609 0 None - 1 Human 9.2 pKi = 9.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 577 11 2 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(C)CNCCCCc2ccnnc2)c1 10.1016/j.bmc.2007.09.026
CHEMBL2371502 208306 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@](C)(Cc2ccc(O)cc2)NC1=O 10.1021/jm990115h
CHEMBL2371484 208299 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCNC(=O)[C@H](Cc3ccccc3)NC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44380258 160698 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
91931283 160698 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL411963 160698 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
10985312 78321 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL21126 78321 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
10985312 78321 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/j.bmc.2007.09.026
CHEMBL21126 78321 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/j.bmc.2007.09.026
CHEMBL2371575 208335 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL405420 210802 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44288080 159629 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 1009 15 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL410940 159629 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 1009 15 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL407800 210927 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44400245 125547 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL364914 125547 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44400245 125547 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL364914 125547 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
11250647 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44400271 68971 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL192912 68971 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL2371549 208325 0 None - 1 Rat 9.0 pKi = 9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm990115h
44432649 86258 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231739 86258 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11365653 173608 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 173608 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10311600 160349 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 523 10 3 9 4.4 CNCCNc1nc(OC)c(NC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)OC4(C)C)o2)c(OC)n1 10.1016/j.bmc.2007.09.026
CHEMBL411526 160349 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 523 10 3 9 4.4 CNCCNc1nc(OC)c(NC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)OC4(C)C)o2)c(OC)n1 10.1016/j.bmc.2007.09.026
CHEMBL385982 210615 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL410357 211058 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCCC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11477988 90565 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm701249f
CHEMBL23969 90565 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm701249f
11477988 90565 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90565 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
21018389 67108 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL189164 67108 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353277 20055 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 712 16 2 7 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL130558 20055 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 712 16 2 7 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
25156943 187843 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL502341 187843 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036877 173068 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 173068 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44340749 108618 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL321376 108618 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
44267868 97611 0 None 10 2 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273275 97611 0 None 10 2 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
9809065 101147 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 611 11 0 9 5.2 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccn1 10.1021/jm0205402
CHEMBL298982 101147 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 611 11 0 9 5.2 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccn1 10.1021/jm0205402
11202636 10120 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL116071 10120 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44353248 19537 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 13 1 8 5.9 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL130126 19537 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 13 1 8 5.9 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
11202636 10120 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL116071 10120 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
21018389 67108 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL189164 67108 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44379167 167188 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL 1376 16 15 15 -1.0 CC(=O)NC1CC(=O)NC(C(=O)N[C@H]2CC(=O)NC(C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)C(Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL430344 167188 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL 1376 16 15 15 -1.0 CC(=O)NC1CC(=O)NC(C(=O)N[C@H]2CC(=O)NC(C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)C(Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371487 208302 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
11331001 188425 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509075 188425 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036878 172467 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 5.9 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL451916 172467 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 5.9 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11365653 173608 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 173608 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11331001 188425 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
CHEMBL509075 188425 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
11262242 188142 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 188142 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44288081 157767 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 13 1 14 8.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL408925 157767 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 13 1 14 8.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44400261 133478 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
CHEMBL371613 133478 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
44400261 133478 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
CHEMBL371613 133478 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
44378649 96693 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1287 27 14 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL267984 96693 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1287 27 14 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
44379259 141060 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1277 24 12 15 -0.4 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
CHEMBL385090 141060 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1277 24 12 15 -0.4 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
44378908 161271 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1273 27 14 15 -2.3 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)N(CC(=O)O)C(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm990115h
CHEMBL414556 161271 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1273 27 14 15 -2.3 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)N(CC(=O)O)C(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm990115h
CHEMBL2371518 208314 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44432635 86342 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 86342 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
11262242 188142 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 188142 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44434386 89364 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL237734 89364 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
86276160 109353 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 485 9 1 8 5.0 COc1nc(OCCF)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
CHEMBL3233521 109353 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 485 9 1 8 5.0 COc1nc(OCCF)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
44400229 68326 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL192171 68326 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371559 208330 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44432636 86943 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 86943 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44432642 153048 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 153048 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44287759 96236 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 999 12 2 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL264043 96236 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 999 12 2 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL407589 210913 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)N[C@@H](C)C(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL410382 211060 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3cccnc3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371538 208321 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44347047 16407 0 None 5 2 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL124056 16407 0 None 5 2 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL264332 208858 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371531 208317 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC1=O 10.1021/jm9901172
CHEMBL412009 211213 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11168776 63264 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL180076 63264 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44400352 67444 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 545 8 1 6 5.1 CCOc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190929 67444 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 545 8 1 6 5.1 CCOc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371539 208322 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](C)NC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44378966 95984 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL262160 95984 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44432650 86330 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
CHEMBL232097 86330 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
44432640 154422 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 154422 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
9854500 101789 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL303274 101789 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
9854500 101789 0 None -2 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 101789 0 None -2 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
9854500 101789 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
CHEMBL303274 101789 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
11331001 188425 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 188425 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44576645 187603 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 571 9 2 8 3.6 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499026 187603 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 571 9 2 8 3.6 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353201 20832 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 15 2 7 6.3 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL131182 20832 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 15 2 7 6.3 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44394589 66571 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 453 6 1 6 4.1 Cc1c(-c2cccs2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL186563 66571 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 453 6 1 6 4.1 Cc1c(-c2cccs2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11752130 14008 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL119808 14008 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL405806 210826 0 None - 1 Rat 8.0 pKi = 8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm990115h
44435979 88099 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235269 88099 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44436017 88290 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 9 0 7 4.7 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236152 88290 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 9 0 7 4.7 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44435993 161120 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 665 10 0 8 5.9 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3C(F)(F)F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL413238 161120 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 665 10 0 8 5.9 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3C(F)(F)F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44347085 15068 0 None -3 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121145 15068 0 None -3 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44587396 172675 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 603 10 2 7 4.9 Cc1c(-c2cccc(OCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL452474 172675 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 603 10 2 7 4.9 Cc1c(-c2cccc(OCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44343914 114298 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL334063 114298 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11330603 128143 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL366865 128143 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL430613 128143 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
11156980 62249 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL178281 62249 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44353229 19975 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 11 1 7 6.5 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130487 19975 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 11 1 7 6.5 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44343914 114298 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL334063 114298 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44309615 102183 0 None - 1 Human 7.0 pKi = 7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(Cl)cc(Cl)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304548 102183 0 None - 1 Human 7.0 pKi = 7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(Cl)cc(Cl)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44435978 88055 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 575 11 0 8 3.5 COc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235051 88055 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 575 11 0 8 3.5 COc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
11284357 60677 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL176270 60677 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL72913 60677 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
44451476 95387 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1535 30 8 18 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL258970 95387 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1535 30 8 18 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44267883 16122 0 None -3 2 Human 5.0 pKi = 5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12265 16122 0 None -3 2 Human 5.0 pKi = 5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11249548 98620 0 None -97 2 Rat 5.0 pKi = 5 Binding
In vivo inhibition of rat Gonadotropin releasing hormone receptorIn vivo inhibition of rat Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98620 0 None -97 2 Rat 5.0 pKi = 5 Binding
In vivo inhibition of rat Gonadotropin releasing hormone receptorIn vivo inhibition of rat Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
44340637 9473 0 None 1479 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards monkey gonadotropin releasing hormone receptorBinding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 9473 0 None 1479 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards monkey gonadotropin releasing hormone receptorBinding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21048269 110595 0 None 2 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326313 110595 0 None 2 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047785 15270 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121576 15270 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11227010 85224 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 12 0 9 3.9 COc1cc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc(OC)c1OC 10.1021/jm030472z
CHEMBL22852 85224 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 12 0 9 3.9 COc1cc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc(OC)c1OC 10.1021/jm030472z
CHEMBL438103 211992 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC1=O 10.1021/jm990116+
9807700 186709 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 8 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL49297 186709 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 8 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44346376 113294 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 10 1 7 7.3 CCNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332463 113294 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 10 1 7 7.3 CCNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44309440 102148 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304308 102148 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44387924 60141 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175465 60141 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047534 16249 0 None 1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL123284 16249 0 None 1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
21047534 16249 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL123284 16249 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL263542 208819 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
12986401 187048 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 464 7 1 7 3.0 COc1cccc(-n2c(=O)c(Cc3c(F)cccc3F)nn(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL494968 187048 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 464 7 1 7 3.0 COc1cccc(-n2c(=O)c(Cc3c(F)cccc3F)nn(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
10226423 188809 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)[C@@H](c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL513126 188809 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)[C@@H](c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
11330034 83966 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2ccc(C(C)C)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22196 83966 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2ccc(C(C)C)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44593613 188064 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL503624 188064 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
44389658 62901 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL179101 62901 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44309541 202167 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 647 12 0 9 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68753 202167 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 647 12 0 9 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44309439 202199 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 630 10 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68988 202199 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 630 10 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
44593613 188064 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.07.059
CHEMBL503624 188064 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.07.059
21045834 16253 0 None 3 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL123301 16253 0 None 3 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44451367 59339 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 6 1 6 4.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4NCCc5ccccc54)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
CHEMBL172192 59339 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 6 1 6 4.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4NCCc5ccccc54)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
9892420 201442 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL64148 201442 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11294757 63492 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL180280 63492 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
44576643 187460 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 512 7 2 6 4.0 NCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL497747 187460 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 512 7 2 6 4.0 NCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
11329628 62680 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
CHEMBL178805 62680 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
CHEMBL73575 62680 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
10983979 201476 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 505 10 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccc3)c2=O)c1 10.1021/jm034041s
CHEMBL64252 201476 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 505 10 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccc3)c2=O)c1 10.1021/jm034041s
44451485 157618 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2cccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL408759 157618 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2cccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11226753 62999 0 None -389 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 62999 0 None -389 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
9984259 109999 0 None -281 2 Rat 5.0 pKi = 5.0 Binding
Tested for binding affinity towards rat gonadotropin releasing hormone receptorTested for binding affinity towards rat gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 109999 0 None -281 2 Rat 5.0 pKi = 5.0 Binding
Tested for binding affinity towards rat gonadotropin releasing hormone receptorTested for binding affinity towards rat gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44267881 17874 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12666 17874 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267876 97642 0 None -53 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273466 97642 0 None -53 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44309511 202544 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 624 13 1 9 5.3 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL71141 202544 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 624 13 1 9 5.3 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
44340788 9436 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112287 9436 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44343804 10457 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 517 10 1 6 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](CC(C)C)NC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116976 10457 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 517 10 1 6 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](CC(C)C)NC(C)C)c2=O)c1F 10.1021/jm049791w
44343779 10904 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL117504 10904 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL2371488 208303 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
25156946 187775 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 11 2 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL501329 187775 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 11 2 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11168634 84650 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 536 10 0 7 4.6 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL22459 84650 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 536 10 0 7 4.6 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
11226753 62999 0 None 389 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 62999 0 None 389 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11180219 110720 0 None 112 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110720 0 None 112 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
44394723 123812 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 468 6 1 7 3.8 Cc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL363659 123812 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 468 6 1 7 3.8 Cc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44400146 67216 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 570 9 1 8 3.0 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL189984 67216 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 570 9 1 8 3.0 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371493 208304 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL265232 208886 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44432627 147584 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL393540 147584 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
44387880 60199 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175821 60199 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44387979 60263 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 8 1 9 2.1 COc1ccccc1Cn1c(=O)n(C[C@H](N)c2ccccc2)c(=O)n(-c2cccc(OC)c2F)c1=O 10.1016/j.bmcl.2005.05.038
CHEMBL176020 60263 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 8 1 9 2.1 COc1ccccc1Cn1c(=O)n(C[C@H](N)c2ccccc2)c(=O)n(-c2cccc(OC)c2F)c1=O 10.1016/j.bmcl.2005.05.038
23450008 131872 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL369723 131872 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
44267904 97951 0 None 6 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275521 97951 0 None 6 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44352734 18314 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL127384 18314 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11443571 164249 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2cccc(F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL421858 164249 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2cccc(F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11168176 122493 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL360910 122493 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL73526 122493 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
21047799 109901 0 None -6 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL324394 109901 0 None -6 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340631 9402 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112131 9402 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
11421412 178154 11 None -2398 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 178154 11 None -2398 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11763365 100720 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 551 7 0 7 5.4 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc4c(n3c2=O)CN(CCc2ccccn2)CC4(C)C)c1 10.1021/jm0205402
CHEMBL295807 100720 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 551 7 0 7 5.4 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc4c(n3c2=O)CN(CCc2ccccn2)CC4(C)C)c1 10.1021/jm0205402
9984259 109999 0 None -281 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 109999 0 None -281 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44309440 102148 0 None - 1 Human 4.9 pKi = 4.9 Binding
Compound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistCompound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304308 102148 0 None - 1 Human 4.9 pKi = 4.9 Binding
Compound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistCompound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44267903 161671 0 None 3 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL416337 161671 0 None 3 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44389652 165460 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 473 6 1 7 3.5 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL425529 165460 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 473 6 1 7 3.5 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1F 10.1016/j.bmcl.2005.01.009
10347081 89066 0 None -223 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 89066 0 None -223 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435817 88661 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 489 6 0 6 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236544 88661 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 489 6 0 6 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL410452 211066 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
CHEMBL438901 212047 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm990116+
44577101 177942 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 532 7 1 7 4.1 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466736 177942 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 532 7 1 7 4.1 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
11249548 98620 0 None 97 2 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98620 0 None 97 2 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
11179420 63004 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 6 4.7 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1021/jm049218c
CHEMBL179460 63004 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 6 4.7 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1021/jm049218c
11341364 165522 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 519 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL425864 165522 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 519 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44388018 60137 0 None 389 2 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60137 0 None 389 2 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
10050123 11063 0 None 20 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117863 11063 0 None 20 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44288074 99751 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 951 13 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL288534 99751 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 951 13 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
11179660 89268 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23767 89268 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
10930118 101476 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 610 11 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccc1 10.1021/jm0205402
CHEMBL301322 101476 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 610 11 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccc1 10.1021/jm0205402
11179660 89268 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL23767 89268 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
44353254 21593 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 574 12 1 7 6.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)C)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL131942 21593 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 574 12 1 7 6.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)C)cc1 10.1016/s0960-894x(01)00780-6
44394651 122397 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 573 8 2 8 5.8 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)c(C)c1 10.1016/j.bmcl.2004.07.022
CHEMBL360625 122397 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 573 8 2 8 5.8 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)c(C)c1 10.1016/j.bmcl.2004.07.022
44394685 126970 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL366127 126970 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
10951713 101765 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL303140 101765 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
44309573 201961 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 625 12 0 9 5.8 CCN(CC)CCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL67370 201961 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 625 12 0 9 5.8 CCN(CC)CCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL405961 210831 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
21045818 112584 0 None 3 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331337 112584 0 None 3 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44388018 60137 0 None -389 2 Rat 4.9 pKi = 4.9 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60137 0 None -389 2 Rat 4.9 pKi = 4.9 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44436014 88144 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 568 7 0 6 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1C1CCCC1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235519 88144 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 568 7 0 6 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1C1CCCC1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44436016 147028 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 688 10 0 8 5.3 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCN(C[C@@H]3CCCN3Cc3ccccn3)C1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL393093 147028 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 688 10 0 8 5.3 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCN(C[C@@H]3CCCN3Cc3ccccn3)C1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44309535 102504 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL306684 102504 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
44379747 96324 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990116+
CHEMBL264806 96324 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990116+
CHEMBL410451 211065 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44577097 177906 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.4 C=C1C(Cl)=CC=C1c1c(C)n(Cc2c(F)cccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm701249f
CHEMBL466531 177906 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.4 C=C1C(Cl)=CC=C1c1c(C)n(Cc2c(F)cccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm701249f
11261693 63063 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
CHEMBL179612 63063 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
CHEMBL74721 63063 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
44353270 114703 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 12 1 8 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL334537 114703 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 12 1 8 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44353230 116273 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 610 13 0 8 6.4 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL337748 116273 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 610 13 0 8 6.4 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44379747 96324 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990118u
CHEMBL264806 96324 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990118u
44394567 65836 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccc(Cl)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL184345 65836 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccc(Cl)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
21047618 114019 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333574 114019 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44267874 96753 0 None 15 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268489 96753 0 None 15 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11283517 94997 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL25714 94997 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11283517 94997 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL25714 94997 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
11330280 122523 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
CHEMBL360934 122523 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
CHEMBL72606 122523 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
21047937 110796 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326606 110796 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44312724 12279 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL1185733 12279 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL430618 12279 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
44309616 202039 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(C(F)(F)F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL67820 202039 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(C(F)(F)F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
25113693 161353 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL415279 161353 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047859 14033 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL119856 14033 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11376064 166575 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL429062 166575 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44400147 67301 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 612 9 1 9 2.7 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N3CCOCC3)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190676 67301 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 612 9 1 9 2.7 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N3CCOCC3)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44309403 202198 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccncc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68985 202198 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccncc2)cc1 10.1016/s0960-894x(02)00371-2
44435994 146498 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 482 8 0 6 3.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)C)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL392688 146498 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 482 8 0 6 3.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)C)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44267811 96754 0 None 14 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268491 96754 0 None 14 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
21047807 112474 0 None -23 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331087 112474 0 None -23 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11249167 89855 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23854 89855 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL216526 207575 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
44435979 88099 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1021/jm701249f
CHEMBL235269 88099 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1021/jm701249f
11249167 89855 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL23854 89855 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm701249f
11214860 84333 0 None 323 2 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84333 0 None 323 2 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
11249167 89855 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23854 89855 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
11192229 122590 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL361128 122590 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11168776 63264 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL180076 63264 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44394661 65764 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccc(Cl)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL183938 65764 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccc(Cl)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44435982 57776 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 12 0 8 4.6 CCSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL16745 57776 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 12 0 8 4.6 CCSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44435986 96045 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 615 10 0 8 5.0 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262579 96045 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 615 10 0 8 5.0 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44587398 188438 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 659 13 1 7 6.3 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@@H](c2ccccc2)N(C)C)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL509267 188438 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 659 13 1 7 6.3 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@@H](c2ccccc2)N(C)C)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11214860 84333 0 None 323 2 Human 7.8 pKi = 7.8 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84333 0 None 323 2 Human 7.8 pKi = 7.8 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
44267812 97639 0 None -64 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 97639 0 None -64 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44394753 122773 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3cccc(C(F)(F)F)c3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL361513 122773 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3cccc(C(F)(F)F)c3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44346261 113357 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 651 10 2 8 5.7 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332570 113357 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 651 10 2 8 5.7 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44340720 9601 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL113183 9601 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309296 201878 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 584 10 0 9 5.1 COCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL66808 201878 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 584 10 0 9 5.1 COCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
21045833 113179 0 None 11 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL332305 113179 0 None 11 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11330072 86495 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23231 86495 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44394835 122105 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 539 7 1 9 3.3 Cc1c(-c2csc(N3CCOCC3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL360384 122105 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 539 7 1 9 3.3 Cc1c(-c2csc(N3CCOCC3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44387885 131761 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 8 2.4 COc1cccc(-n2c(=O)n(CC[C@H](N)CC(C)C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL369706 131761 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 8 2.4 COc1cccc(-n2c(=O)n(CC[C@H](N)CC(C)C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44341075 9800 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 427 5 1 6 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCNC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114370 9800 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 427 5 1 6 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCNC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44353266 116574 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 635 14 2 6 6.9 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL339273 116574 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 635 14 2 6 6.9 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
21045817 114039 0 None -22 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333730 114039 0 None -22 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44587401 187640 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 14 3 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL499442 187640 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 14 3 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21048323 167138 0 None -8 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL430250 167138 0 None -8 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44435819 88751 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 490 6 0 7 3.3 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccncc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236750 88751 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 490 6 0 7 3.3 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccncc2)CC3)c1 10.1016/j.bmc.2007.05.029
11225960 10891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL117396 10891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
11225960 10891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL117396 10891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
44346375 15175 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 690 9 1 7 7.3 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)C(F)(F)F)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL121441 15175 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 690 9 1 7 7.3 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)C(F)(F)F)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
9891852 9985 0 None 23 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115482 9985 0 None 23 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9959327 101473 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 9 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL301285 101473 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 9 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44394714 122100 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 590 9 2 10 5.1 Cc1c(-c2csc(Nc3ccc([N+](=O)[O-])cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL360363 122100 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 590 9 2 10 5.1 Cc1c(-c2csc(Nc3ccc([N+](=O)[O-])cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
10347081 89066 0 None 223 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 89066 0 None 223 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44436009 88917 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccc5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236966 88917 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccc5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340845 9762 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114183 9762 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44432656 158600 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL409825 158600 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451397 95445 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259220 95445 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44434373 89603 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238160 89603 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44267881 17874 0 None -14 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12666 17874 0 None -14 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL406628 210859 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL415179 211420 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC1=O 10.1021/jm990116+
44353276 116711 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 697 15 2 6 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL339468 116711 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 697 15 2 6 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
44346479 113613 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 11 1 7 7.9 CC(C)CNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332837 113613 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 11 1 7 7.9 CC(C)CNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44435977 88284 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236127 88284 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
9911446 10666 0 None 33 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117170 10666 0 None 33 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340785 114292 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL334037 114292 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11467328 86303 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 9 0 7 5.8 Cc1c(-c2ccc3oc4ccccc4c3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23198 86303 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 9 0 7 5.8 Cc1c(-c2ccc3oc4ccccc4c3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44346398 14354 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL120260 14354 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44346663 114304 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 592 10 0 9 5.2 COCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL334110 114304 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 592 10 0 9 5.2 COCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44451396 156120 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406958 156120 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047815 14764 0 None 30 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120834 14764 0 None 30 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11733484 186252 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 476 6 0 6 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)C)n3c2=O)c1 10.1021/jm0205402
CHEMBL48944 186252 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 476 6 0 6 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)C)n3c2=O)c1 10.1021/jm0205402
11168176 122493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL360910 122493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL73526 122493 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
10874838 100338 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 10 0 7 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL293247 100338 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 10 0 7 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
44435998 145750 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 522 6 0 6 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392087 145750 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 522 6 0 6 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
21047631 10843 0 None 5 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117330 10843 0 None 5 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44346848 112558 0 None 1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331204 112558 0 None 1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
21045833 113179 0 None -11 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL332305 113179 0 None -11 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11318370 9595 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113151 9595 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44394857 123826 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 7 1 7 5.4 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL363731 123826 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 7 1 7 5.4 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44400204 167982 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 2 6 4.4 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL435689 167982 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 2 6 4.4 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44309390 167547 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)cc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL432922 167547 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)cc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44432628 87313 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 87313 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
44387961 165457 0 None 144 2 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165457 0 None 144 2 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267864 167184 0 None 30 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
CHEMBL430312 167184 0 None 30 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
44267902 97939 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL275467 97939 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44287893 162642 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 919 11 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL418256 162642 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 919 11 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267902 97939 0 None -6 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275467 97939 0 None -6 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44352665 117758 0 None 43 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340934 117758 0 None 43 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11319703 122566 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 529 7 1 6 5.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1SC(F)(F)F 10.1021/jm049218c
CHEMBL361016 122566 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 529 7 1 6 5.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1SC(F)(F)F 10.1021/jm049218c
15462666 96042 4 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL262557 96042 4 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44435996 88343 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 9 0 7 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236342 88343 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 9 0 7 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44387926 130080 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 528 8 1 8 3.2 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3Cl)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL368153 130080 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 528 8 1 8 3.2 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3Cl)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
21047799 109901 0 None 6 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL324394 109901 0 None 6 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21048323 167138 0 None 8 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL430250 167138 0 None 8 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9851194 116171 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 578 10 0 8 5.6 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL337172 116171 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 578 10 0 8 5.6 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44341057 162793 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL419212 162793 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435995 88287 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 524 9 0 6 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236137 88287 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 524 9 0 6 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340649 109134 0 None - 1 Human 4.8 pKi = 4.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL322283 109134 0 None - 1 Human 4.8 pKi = 4.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
11214294 121668 0 None -912 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121668 0 None -912 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11467134 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
CHEMBL361798 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
CHEMBL74686 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
44400099 126891 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 509 8 1 7 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3SC)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL366020 126891 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 509 8 1 7 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3SC)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
10962804 101312 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 566 9 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL300080 101312 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 566 9 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
44448991 154790 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154790 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154790 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44353246 20006 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 538 9 1 7 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130513 20006 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 538 9 1 7 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44340635 9583 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL113068 9583 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
44288078 156527 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 910 11 2 14 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL40743 156527 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 910 11 2 14 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL317064 209441 13 None - 1 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44451349 95692 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCNCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
CHEMBL260540 95692 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCNCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
44434438 145650 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392008 145650 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44267875 15379 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12204 15379 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
10323198 123832 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL363759 123832 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
10323198 123832 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL363759 123832 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44432657 148923 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394613 148923 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11671279 130349 0 None 331 2 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130349 0 None 331 2 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44353262 116302 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL337919 116302 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
25156400 188262 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL506877 188262 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036877 173068 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 173068 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44267876 97642 0 None 53 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273466 97642 0 None 53 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11331001 188425 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 188425 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
1179 945 31 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 945 31 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 945 31 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL2371556 208327 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCCNC(=O)CCNC(=O)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371558 208329 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL439470 212083 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
11282957 121806 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL359894 121806 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
16058727 193141 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 548 7 1 7 4.6 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
CHEMBL539167 193141 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 548 7 1 7 4.6 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
11282957 121806 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121806 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
11282957 121806 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL359894 121806 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL2371498 208305 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)C(C)(C)OC(C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
71459935 78533 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 466 7 1 4 4.5 COc1cccc(N2CN(Cc3c(F)cccc3F)C(=O)N(C[C@H](N)c3ccccc3)C2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL2113012 78533 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 466 7 1 4 4.5 COc1cccc(N2CN(Cc3c(F)cccc3F)C(=O)N(C[C@H](N)c3ccccc3)C2=O)c1 10.1016/j.bmcl.2004.11.026
11466452 114225 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL333850 114225 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL2371560 208331 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL410819 211089 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@@H]2C(=O)NCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O)C(=O)O 10.1021/jm990115h
44347085 15068 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121145 15068 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44400350 126462 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 6 1 5 5.5 Cc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c(Cl)c1 10.1016/j.bmcl.2005.03.057
CHEMBL365561 126462 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 6 1 5 5.5 Cc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c(Cl)c1 10.1016/j.bmcl.2005.03.057
44432641 166931 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL429976 166931 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
9831160 162906 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL419998 162906 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
9831160 162906 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL419998 162906 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL385505 210596 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCCN)N(C(C)C)C(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3cccnc3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11168311 165678 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL426783 165678 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
10077844 103295 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 637 13 1 8 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL308910 103295 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 637 13 1 8 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44267869 97655 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)O[C@H](C)[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273535 97655 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)O[C@H](C)[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267902 97939 0 None 6 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275467 97939 0 None 6 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL405265 210795 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Affinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
10919567 98560 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL280213 98560 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
10347081 89066 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
CHEMBL23730 89066 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
11467134 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
CHEMBL361798 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
CHEMBL74686 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
11272935 131252 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL369326 131252 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL75954 131252 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
44449186 95095 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL257599 95095 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
44394615 125351 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 572 7 1 8 5.1 Cc1c(-c2csc(-c3ccc4c(c3)CCO4)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL364840 125351 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 572 7 1 8 5.1 Cc1c(-c2csc(-c3ccc4c(c3)CCO4)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
10007333 9496 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112559 9496 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
10347081 89066 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 89066 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
10098618 110829 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL326804 110829 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11467134 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL361798 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL74686 123023 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
44379092 157296 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1337 26 15 14 -0.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL408372 157296 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1337 26 15 14 -0.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44435975 91733 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 11 0 7 4.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL242399 91733 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 11 0 7 4.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44436015 147026 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 8 0 7 4.6 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1Cc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL393092 147026 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 8 0 7 4.6 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1Cc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44387907 60342 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 516 7 1 8 2.5 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL176056 60342 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 516 7 1 8 2.5 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44387992 62181 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 496 7 1 8 2.7 COc1cccc(-n2c(=O)n(Cc3ccccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL178218 62181 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 496 7 1 8 2.7 COc1cccc(-n2c(=O)n(Cc3ccccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21045797 170025 0 None 12 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL445074 170025 0 None 12 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL2371581 208339 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
9984259 109999 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 109999 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44343975 10462 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 586 11 0 8 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL116988 10462 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 586 11 0 8 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
11238637 67215 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 585 6 1 5 6.3 N[C@@H](Cn1c(=O)c(-c2ccc(C(F)(F)F)cc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL189964 67215 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 585 6 1 5 6.3 N[C@@H](Cn1c(=O)c(-c2ccc(C(F)(F)F)cc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11330280 122523 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL360934 122523 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL72606 122523 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
9983568 98512 0 None 263 2 Human 6.7 pKi = 6.7 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98512 0 None 263 2 Human 6.7 pKi = 6.7 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
9984259 109999 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Tested for binding affinity towards monkey gonadotropin releasing hormone receptorTested for binding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 109999 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Tested for binding affinity towards monkey gonadotropin releasing hormone receptorTested for binding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44352801 20128 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL130607 20128 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44340670 9535 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112730 9535 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL317341 209446 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44287779 141030 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 979 12 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL384920 141030 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 979 12 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
21046762 10461 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116986 10461 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267885 17624 0 None -9 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12589 17624 0 None -9 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267811 96754 0 None -14 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268491 96754 0 None -14 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44380024 168456 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
91931289 168456 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
CHEMBL439439 168456 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
CHEMBL407855 210932 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
11490288 168071 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
CHEMBL436276 168071 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
CHEMBL75439 168071 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
44353304 18811 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 2 7 6.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL128810 18811 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 2 7 6.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL2371498 208305 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)C(C)(C)OC(C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
11354193 95754 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 640 9 1 8 3.8 COc1ccc(CN2CC3CC(c4ccc(N(C)C)c5ccccc45)N4C(=O)N(CCN5CCOCC5)C(=O)C34C2)cc1NC(C)=O 10.1016/j.bmc.2007.09.026
CHEMBL260816 95754 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 640 9 1 8 3.8 COc1ccc(CN2CC3CC(c4ccc(N(C)C)c5ccccc45)N4C(=O)N(CCN5CCOCC5)C(=O)C34C2)cc1NC(C)=O 10.1016/j.bmc.2007.09.026
44340783 167325 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL431248 167325 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44394577 122693 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL361313 122693 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44352513 117584 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 11 0 10 4.9 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCOC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL340677 117584 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 11 0 10 4.9 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCOC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44340637 9473 0 None -1479 2 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards rat GnRH gonadotropin releasing hormone receptorBinding affinity towards rat GnRH gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 9473 0 None -1479 2 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards rat GnRH gonadotropin releasing hormone receptorBinding affinity towards rat GnRH gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44267874 96753 0 None -15 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268489 96753 0 None -15 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
21047785 15270 0 None -20 2 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121576 15270 0 None -20 2 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44267885 17624 0 None 9 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12589 17624 0 None 9 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11191153 193191 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL540207 193191 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
44576679 192825 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 12 2 7 4.3 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL526327 192825 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 12 2 7 4.3 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
21047516 15158 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL121412 15158 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
44267810 97627 0 None -5 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL273387 97627 0 None -5 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267810 97627 0 None -5 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273387 97627 0 None -5 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44577067 192624 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 5 1 6 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL523709 192624 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 5 1 6 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1021/jm701249f
11352630 88266 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 504 9 0 6 4.2 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23604 88266 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 504 9 0 6 4.2 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
22716564 123260 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 5 1 6 4.4 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL362283 123260 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 5 1 6 4.4 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
10994908 162446 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 518 10 0 6 4.4 CCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL417558 162446 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 518 10 0 6 4.4 CCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
44309321 202146 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL68625 202146 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
21046762 10461 0 None 9 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116986 10461 0 None 9 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047538 14374 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 555 8 3 6 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(F)c(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120397 14374 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 555 8 3 6 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(F)c(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44390769 64525 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 486 6 1 7 2.5 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL182145 64525 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 486 6 1 7 2.5 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
44309323 202341 0 None - 1 Human 5.7 pKi = 5.7 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 601 12 1 8 6.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN2CCCC2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL69914 202341 0 None - 1 Human 5.7 pKi = 5.7 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 601 12 1 8 6.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN2CCCC2)cc1 10.1016/s0960-894x(02)00370-0
44352735 117930 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 647 14 0 10 6.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL341124 117930 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 647 14 0 10 6.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11071561 101968 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 11 0 7 4.1 CCc1c(-c2cccc(OC)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL304002 101968 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 11 0 7 4.1 CCc1c(-c2cccc(OC)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44435820 160782 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 542 7 1 6 4.4 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(CCc2c[nH]c4ccccc24)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL412581 160782 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 542 7 1 6 4.4 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(CCc2c[nH]c4ccccc24)CC3)c1 10.1016/j.bmc.2007.05.029
44451460 155895 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)c2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406713 155895 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)c2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11191675 63037 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63037 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63037 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
9958318 89782 0 None -15 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89782 0 None -15 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL266536 208932 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44577051 186837 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 509 7 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)(N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL493794 186837 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 509 7 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)(N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44344157 110875 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 543 9 1 6 5.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL327076 110875 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 543 9 1 6 5.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
44434404 166004 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL427981 166004 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44309582 202492 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 569 11 0 9 4.6 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL70851 202492 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 569 11 0 9 4.6 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00370-0
44389658 62901 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL179101 62901 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
12991507 186983 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 461 5 1 6 3.6 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1021/jm701249f
CHEMBL494621 186983 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 461 5 1 6 3.6 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1021/jm701249f
10940289 90203 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23900 90203 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44312821 11943 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL1183624 11943 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL308154 11943 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
11330603 128143 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL366865 128143 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL430613 128143 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
22716524 123126 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 461 5 1 6 3.6 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL362025 123126 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 461 5 1 6 3.6 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
10940289 90203 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm034041s
CHEMBL23900 90203 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm034041s
44309525 102786 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 611 13 0 9 5.8 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00371-2
CHEMBL308446 102786 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 611 13 0 9 5.8 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00371-2
10557573 110946 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 870 22 9 8 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C1=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL327528 110946 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 870 22 9 8 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C1=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
11671279 130349 0 None -331 2 Rat 5.6 pKi = 5.6 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130349 0 None -331 2 Rat 5.6 pKi = 5.6 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44346848 112558 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331204 112558 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
10929667 85331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22929 85331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
10929667 85331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL22929 85331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44388002 121859 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CC[C@H](N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL360047 121859 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CC[C@H](N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047784 110135 0 None 36 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL325747 110135 0 None 36 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21046570 112575 0 None 34 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL331277 112575 0 None 34 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
11671279 130349 0 None 331 2 Human 7.6 pKi = 7.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130349 0 None 331 2 Human 7.6 pKi = 7.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
10929667 85331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmc.2007.09.026
CHEMBL22929 85331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmc.2007.09.026
44340780 9642 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 543 13 0 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113455 9642 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 543 13 0 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
10929574 100652 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 538 8 1 6 6.3 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL295275 100652 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 538 8 1 6 6.3 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
11421243 90215 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2cccc(C(C)C)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23908 90215 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2cccc(C(C)C)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
21048269 110595 0 None -2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326313 110595 0 None -2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11123821 201607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 491 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccc3)c2=O)c1 10.1021/jm034041s
CHEMBL64795 201607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 491 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccc3)c2=O)c1 10.1021/jm034041s
44387961 165457 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165457 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44352548 167998 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cccc(F)c2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL435793 167998 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cccc(F)c2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44343932 167996 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 561 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL435784 167996 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 561 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
44436004 88304 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236197 88304 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44436005 88672 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCNC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236550 88672 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCNC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
10439527 168902 0 None 288 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL443027 168902 0 None 288 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11477970 89055 0 None 281 2 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89055 0 None 281 2 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44436002 146551 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392731 146551 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340784 9397 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112093 9397 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21045797 170025 0 None -12 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL445074 170025 0 None -12 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340804 9045 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL110052 9045 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
9825757 109656 0 None 12 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323687 109656 0 None 12 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340636 110740 0 None - 1 Human 5.6 pKi = 5.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL326510 110740 0 None - 1 Human 5.6 pKi = 5.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
44352514 18674 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 659 13 0 9 6.3 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C4CC4)C4CC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL128262 18674 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 659 13 0 9 6.3 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C4CC4)C4CC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44309252 202128 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 589 9 0 7 5.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(Br)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68537 202128 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 589 9 0 7 5.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(Br)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44451385 95618 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 580 10 0 7 4.4 CC(C)CN(C)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(OC(F)(F)F)cc1)C2 10.1016/j.bmc.2007.09.026
CHEMBL260058 95618 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 580 10 0 7 4.4 CC(C)CN(C)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(OC(F)(F)F)cc1)C2 10.1016/j.bmc.2007.09.026
11477970 89055 0 None -281 2 Rat 4.6 pKi = 4.6 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89055 0 None -281 2 Rat 4.6 pKi = 4.6 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44267883 16122 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12265 16122 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44435985 146405 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392604 146405 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2007.05.029
44436008 88916 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.2 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(C5CCCC5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236965 88916 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.2 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(C5CCCC5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44435999 146553 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392733 146553 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44394818 165555 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 530 7 1 7 5.1 Cc1c(-c2csc(-c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL426058 165555 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 530 7 1 7 5.1 Cc1c(-c2csc(-c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
21045828 14380 0 None 2 2 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120420 14380 0 None 2 2 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352515 116557 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 633 11 0 9 6.0 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL339211 116557 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 633 11 0 9 6.0 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
11766904 186049 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 561 11 0 7 5.7 CCN(CC)CCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL48806 186049 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 561 11 0 7 5.7 CCN(CC)CCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
44312666 11949 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL1183666 11949 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL310716 11949 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
44451319 95715 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260647 95715 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352874 22102 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 575 11 0 9 4.9 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132387 22102 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 575 11 0 9 4.9 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44343976 10463 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 571 10 0 7 5.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL116989 10463 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 571 10 0 7 5.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
11319401 121616 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL359681 121616 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
11261693 63063 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL179612 63063 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL74721 63063 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
44587399 188027 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 646 13 3 8 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL502967 188027 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 646 13 3 8 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44387908 62844 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 500 8 1 9 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3cccs3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL179023 62844 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 500 8 1 9 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3cccs3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44287778 81154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 15 2 14 7.8 CCC(C)N(CC1CC1)[C@H]1C[C@@H](C)OC(O[C@@H]2[C@@H](C)[C@H](OC3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@]3(C)OC(=O)N(CCc4ccc(Cl)cc4)[C@@H]3[C@@H](C)C(=O)[C@H](C)C[C@]2(C)OC)[C@@H]1O 10.1016/j.bmcl.2003.12.059
CHEMBL216252 81154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 15 2 14 7.8 CCC(C)N(CC1CC1)[C@H]1C[C@@H](C)OC(O[C@@H]2[C@@H](C)[C@H](OC3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@]3(C)OC(=O)N(CCc4ccc(Cl)cc4)[C@@H]3[C@@H](C)C(=O)[C@H](C)C[C@]2(C)OC)[C@@H]1O 10.1016/j.bmcl.2003.12.059
44353264 22036 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 10 0 9 5.5 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(C3=NC(C)(C)CO3)c(=O)n12 10.1016/s0960-894x(01)00780-6
CHEMBL132339 22036 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 10 0 9 5.5 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(C3=NC(C)(C)CO3)c(=O)n12 10.1016/s0960-894x(01)00780-6
10050123 11063 0 None -20 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117863 11063 0 None -20 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44394852 126631 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 497 8 2 8 3.9 CCNc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL365695 126631 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 497 8 2 8 3.9 CCNc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44346374 113917 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333233 113917 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
21045823 113630 0 None -40 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL332923 113630 0 None -40 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21046387 110150 0 None -53 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL325843 110150 0 None -53 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44267863 98053 0 None 2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL276217 98053 0 None 2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44387935 61755 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(CN)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL177523 61755 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(CN)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
44347004 15260 0 None 13 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121535 15260 0 None 13 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340798 108287 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL320920 108287 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21047859 14033 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL119856 14033 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340644 9806 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 517 7 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(Cc4ccccc4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114399 9806 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 517 7 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(Cc4ccccc4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309399 202196 0 None - 1 Human 4.6 pKi = 4.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 518 10 1 7 5.4 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OC(CC)CC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL68964 202196 0 None - 1 Human 4.6 pKi = 4.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 518 10 1 7 5.4 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OC(CC)CC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
44352566 20443 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3cccnc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL130861 20443 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3cccnc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44309361 102249 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 7 0 9 4.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCOCC2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304950 102249 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 7 0 9 4.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCOCC2)cc1 10.1016/s0960-894x(02)00371-2
44309585 202664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 641 14 1 9 6.7 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccco2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL71793 202664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 641 14 1 9 6.7 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccco2)cc1 10.1016/s0960-894x(02)00370-0
44587405 171664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 673 13 2 7 6.6 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCC(C)(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL447424 171664 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 673 13 2 7 6.6 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCC(C)(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44387918 60321 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 476 7 1 8 2.4 COc1cccc(-n2c(=O)n(Cc3ccccc3C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL176029 60321 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 476 7 1 8 2.4 COc1cccc(-n2c(=O)n(Cc3ccccc3C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047519 14286 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
CHEMBL120048 14286 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
44434411 146208 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392434 146208 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44309375 103129 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 11 1 8 7.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2N2CCC3C=CC=CC3C2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL308696 103129 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 11 1 8 7.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2N2CCC3C=CC=CC3C2)cc1 10.1016/s0960-894x(02)00370-0
10345138 122029 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122029 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122029 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
11226470 162507 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 538 10 0 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL417645 162507 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 538 10 0 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1F 10.1021/jm030472z
10027591 125737 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 467 6 1 6 4.4 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)s1 10.1016/j.bmcl.2004.07.022
CHEMBL365012 125737 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 467 6 1 6 4.4 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)s1 10.1016/j.bmcl.2004.07.022
44387977 60181 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 548 7 1 8 3.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175711 60181 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 548 7 1 8 3.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44347048 14329 0 None 18 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120164 14329 0 None 18 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL438374 212009 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11375759 63489 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 5 4.5 Cc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL180262 63489 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 5 4.5 Cc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
11444886 122102 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
CHEMBL308289 122102 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
CHEMBL360367 122102 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
11467552 172132 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 172132 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11282957 121806 0 None 1096 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2008.04.029
CHEMBL359894 121806 0 None 1096 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2008.04.029
44576644 188378 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 7 5.0 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)C3CC3)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL508435 188378 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 7 5.0 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)C3CC3)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353285 117218 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 678 17 2 7 7.1 CCCCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL340156 117218 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 678 17 2 7 7.1 CCCCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL2371585 208343 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44378834 96367 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1291 24 12 15 -0.1 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
CHEMBL265169 96367 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1291 24 12 15 -0.1 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
11455317 62544 0 None 851 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62544 0 None 851 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11467552 172132 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 172132 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44576680 172959 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 627 13 2 9 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL453167 172959 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 627 13 2 9 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
11167850 2691 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2691 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2691 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2691 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
11191675 63037 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL179600 63037 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL3085404 63037 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
11456285 188337 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 613 12 2 8 4.1 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
CHEMBL508020 188337 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 613 12 2 8 4.1 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
44379006 168377 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1257 22 13 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)NC1=O 10.1021/jm990115h
CHEMBL438899 168377 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1257 22 13 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)NC1=O 10.1021/jm990115h
11421518 164733 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
CHEMBL423291 164733 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
44449095 154959 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL404180 154959 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
25156942 188072 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](c3ccccc3)N(C)CCCC(=O)O)c2=O)c1F 10.1021/jm8006454
CHEMBL503705 188072 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](c3ccccc3)N(C)CCCC(=O)O)c2=O)c1F 10.1021/jm8006454
1179 945 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
9957278 945 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
CHEMBL494803 945 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
44353258 115567 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 14 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL335647 115567 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 14 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
1179 945 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 945 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 945 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
44267868 97611 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL273275 97611 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
11421518 164733 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164733 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44388511 123137 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 515 6 1 5 5.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cc(F)ccc1C(F)(F)F 10.1021/jm049218c
CHEMBL362065 123137 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 515 6 1 5 5.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cc(F)ccc1C(F)(F)F 10.1021/jm049218c
9850211 187684 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL50009 187684 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
10886383 199213 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL60153 199213 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
44394901 66015 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccccc3Cl)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL185154 66015 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccccc3Cl)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44400246 67299 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 569 9 1 8 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)C(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190671 67299 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 569 9 1 8 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)C(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
10886383 199213 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL60153 199213 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44436003 88288 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236142 88288 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44435980 146402 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392602 146402 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2007.05.029
11421518 164733 0 None 1047 2 Human 7.5 pKi = 7.5 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164733 0 None 1047 2 Human 7.5 pKi = 7.5 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44309376 202397 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 600 13 1 9 5.4 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CC#N)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL70276 202397 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 600 13 1 9 5.4 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CC#N)cc1 10.1016/s0960-894x(02)00370-0
10929801 101454 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 564 11 0 9 4.2 COCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL301103 101454 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 564 11 0 9 4.2 COCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
44346349 113458 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 679 12 2 8 6.5 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332616 113458 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 679 12 2 8 6.5 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44435976 88054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 601 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(C)(C)C)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235050 88054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 601 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(C)(C)C)cc1)C2 10.1016/j.bmc.2007.05.029
21047805 113938 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 588 10 2 7 7.0 COc1cc(OC)nc(NCC2CCC(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)CC2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL333349 113938 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 588 10 2 7 7.0 COc1cc(OC)nc(NCC2CCC(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)CC2)n1 10.1016/s0960-894x(02)00756-4
11167850 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1178 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1187 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL179691 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
11167850 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2691 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
9825757 109656 0 None -12 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323687 109656 0 None -12 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44394893 129135 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 469 6 2 8 3.1 Cc1c(-c2csc(N)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367369 129135 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 469 6 2 8 3.1 Cc1c(-c2csc(N)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44451418 168141 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1620 32 9 19 8.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@H](C)NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436878 168141 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1620 32 9 19 8.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@H](C)NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44309522 96066 0 None - 1 Human 4.5 pKi = 4.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 476 8 1 7 4.3 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OCC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL262787 96066 0 None - 1 Human 4.5 pKi = 4.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 476 8 1 7 4.3 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OCC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
44435991 146410 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 8 4.7 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL392607 146410 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 8 4.7 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44352652 116968 0 None 245 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL339968 116968 0 None 245 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL2371532 208318 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371584 208342 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44340825 167507 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL432585 167507 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44400255 134194 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 577 7 1 7 4.5 CS(=O)(=O)c1cccc(C(F)(F)F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
CHEMBL371855 134194 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 577 7 1 7 4.5 CS(=O)(=O)c1cccc(C(F)(F)F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
44340808 110065 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325326 110065 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44593615 174039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL455769 174039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353200 20754 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 676 13 2 7 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL131127 20754 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 676 13 2 7 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44593615 174039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL455769 174039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
10995320 187577 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 562 11 0 8 5.4 CCCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL49872 187577 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 562 11 0 8 5.4 CCCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11785958 86597 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
CHEMBL23256 86597 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
11785958 86597 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23256 86597 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44327851 110947 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 872 11 9 8 3.3 CC[C@H](C)[C@@H]1NC(=O)CSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
CHEMBL327529 110947 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 872 11 9 8 3.3 CC[C@H](C)[C@@H]1NC(=O)CSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
11180219 110720 0 None -112 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110720 0 None -112 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11226531 99046 0 None -169 2 Rat 5.5 pKi = 5.5 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99046 0 None -169 2 Rat 5.5 pKi = 5.5 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44451331 159322 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 8 1 6 4.8 NC(CC1CCCCC1)Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.09.026
CHEMBL410680 159322 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 8 1 6 4.8 NC(CC1CCCCC1)Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.09.026
21048462 109815 0 None -60 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323863 109815 0 None -60 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44352657 21336 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
CHEMBL131665 21336 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
24857895 154769 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL403081 154769 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44394768 123851 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 605 10 2 10 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1OC 10.1016/j.bmcl.2004.07.022
CHEMBL363900 123851 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 605 10 2 10 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1OC 10.1016/j.bmcl.2004.07.022
11490288 168071 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL436276 168071 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL75439 168071 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
44587392 169964 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 13 2 7 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL444989 169964 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 13 2 7 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21045805 13657 0 None -5 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL119546 13657 0 None -5 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
21045829 112886 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331855 112886 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340771 9608 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113216 9608 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44451398 168119 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1676 34 9 19 9.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H](NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)C(C)C)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436697 168119 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1676 34 9 19 9.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H](NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)C(C)C)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
9958318 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23830 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44577096 178153 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 10 0 7 3.7 COc1cccc(-c2c(F)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL468546 178153 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 10 0 7 3.7 COc1cccc(-c2c(F)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
9958318 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44394649 129637 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 1 8 5.2 Cc1c(-c2csc(N(C)c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367812 129637 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 1 8 5.2 Cc1c(-c2csc(N(C)c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9958318 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm049791w
CHEMBL23830 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm049791w
9958318 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23830 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
9892420 201442 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL64148 201442 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1021/jm034041s
44587391 171988 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.4 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL448656 171988 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.4 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
9958318 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL23830 89782 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
11352834 88747 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 516 10 0 6 4.5 C=Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23673 88747 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 516 10 0 6 4.5 C=Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44394614 66593 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 9 2 8 5.1 Cc1c(-c2csc(NCc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL186646 66593 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 9 2 8 5.1 Cc1c(-c2csc(NCc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11272935 131252 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL369326 131252 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL75954 131252 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
44435829 88145 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235520 88145 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44587402 172126 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 674 14 2 8 5.1 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL450414 172126 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 674 14 2 8 5.1 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21047518 15261 0 None 10 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121551 15261 0 None 10 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11145953 183408 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 10 1 7 5.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CNCCc4ccccn4)cn3c2=O)c1 10.1021/jm0205402
CHEMBL48193 183408 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 10 1 7 5.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CNCCc4ccccn4)cn3c2=O)c1 10.1021/jm0205402
CHEMBL2371565 208332 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44309576 101785 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 619 15 1 9 5.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCOC)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL303260 101785 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 619 15 1 9 5.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCOC)cc1 10.1016/s0960-894x(02)00370-0
10919052 113007 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332138 113007 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44387988 131310 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 530 7 1 8 3.4 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL369453 131310 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 530 7 1 8 3.4 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267866 96652 0 None -4 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL267568 96652 0 None -4 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44346260 114313 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 11 2 8 6.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL334148 114313 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 11 2 8 6.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
11225384 127970 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL366701 127970 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
11225384 127970 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL366701 127970 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
11225384 127970 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL366701 127970 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
11375912 84785 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 0 6 4.5 Cc1c(-c2cccc(Cl)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22559 84785 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 0 6 4.5 Cc1c(-c2cccc(Cl)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11260648 167463 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL432262 167463 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
11260648 167463 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL432262 167463 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309372 202156 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 677 13 0 10 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(OC)c(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68698 202156 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 677 13 0 10 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(OC)c(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44347004 15260 0 None -13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121535 15260 0 None -13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352933 21278 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL131589 21278 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44576657 187654 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 587 10 2 7 4.9 N[C@@H](Cn1c(=O)c(-c2ccc(CSCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499589 187654 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 587 10 2 7 4.9 N[C@@H](Cn1c(=O)c(-c2ccc(CSCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11005990 89479 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23797 89479 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11005990 89479 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL23797 89479 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44587404 188443 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 661 14 2 8 5.2 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL509347 188443 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 661 14 2 8 5.2 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44267868 97611 0 None -10 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273275 97611 0 None -10 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44435990 96046 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 585 10 0 8 5.2 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3CC3CCCCC3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262580 96046 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 585 10 0 8 5.2 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3CC3CCCCC3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44451342 96005 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262334 96005 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047518 15261 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121551 15261 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44390795 121651 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 539 7 2 7 2.8 NC(Cc1c[nH]c2ccccc12)Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O 10.1016/j.bmcl.2004.11.026
CHEMBL359741 121651 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 539 7 2 7 2.8 NC(Cc1c[nH]c2ccccc12)Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O 10.1016/j.bmcl.2004.11.026
11113778 201423 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 495 10 2 7 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3c[nH]cn3)c2=O)c1 10.1021/jm034041s
CHEMBL64066 201423 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 495 10 2 7 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3c[nH]cn3)c2=O)c1 10.1021/jm034041s
9891852 9985 0 None -23 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115482 9985 0 None -23 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11178994 10289 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL116259 10289 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
11178994 10289 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116259 10289 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
44593614 187669 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499849 187669 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44593614 187669 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL499849 187669 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11226531 99046 0 None 169 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99046 0 None 169 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44353228 19874 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 622 12 1 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130400 19874 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 622 12 1 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44400187 134747 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 551 6 1 5 5.6 N[C@@H](Cn1c(=O)c(-c2ccccc2C(F)(F)F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL372680 134747 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 551 6 1 5 5.6 N[C@@H](Cn1c(=O)c(-c2ccccc2C(F)(F)F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11444886 122102 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
CHEMBL308289 122102 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
CHEMBL360367 122102 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
10649568 14382 0 None -10 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
CHEMBL120432 14382 0 None -10 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
9983568 98512 0 None 263 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98512 0 None 263 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
11283954 13967 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 8 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL119774 13967 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 8 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
44346667 113231 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332355 113231 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44587393 172055 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449468 172055 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10995569 101201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccn1 10.1021/jm0205402
CHEMBL299348 101201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccn1 10.1021/jm0205402
44449156 154493 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL401632 154493 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL2371583 208341 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371479 208297 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H]1NC(=O)CC[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](Cc3cccnc3)NC(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(C)=O)CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCNC1=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC2=O 10.1021/jm990115h
25156944 188513 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 8 5.6 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/jm8006454
CHEMBL510285 188513 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 8 5.6 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/jm8006454
44577098 177939 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 539 8 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3[S+](C)[O-])c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466730 177939 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 539 8 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3[S+](C)[O-])c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44267810 97627 0 None 5 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273387 97627 0 None 5 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11214614 188829 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1021/jm701249f
CHEMBL513346 188829 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1021/jm701249f
10051739 84994 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 84994 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
10051739 84994 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL22653 84994 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44449682 95587 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 533 8 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1 10.1016/j.bmcl.2008.04.029
CHEMBL259907 95587 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 533 8 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1 10.1016/j.bmcl.2008.04.029
10051739 84994 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL22653 84994 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm049791w
22716581 121995 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1016/j.bmcl.2005.01.009
CHEMBL360126 121995 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1016/j.bmcl.2005.01.009
44432638 86343 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 86343 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
11490509 63019 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 5 4.6 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Br 10.1021/jm049218c
CHEMBL179531 63019 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 5 4.6 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Br 10.1021/jm049218c
9986320 100951 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human Gonadotropin-releasing hormone receptorBinding affinity to human Gonadotropin-releasing hormone receptor
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm0205402
CHEMBL297491 100951 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human Gonadotropin-releasing hormone receptorBinding affinity to human Gonadotropin-releasing hormone receptor
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm0205402
9986320 100951 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL297491 100951 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL2371555 208326 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H]2CC(=O)N[C@H](C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H]3CCCCNC(=O)CC[C@H](NC2=O)C(=O)N[C@H](Cc2ccc4ccccc4c2)C(=O)N[C@@H](CC(C)C)C(=O)N3)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
10394119 113936 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards rat pituitary Gonadotropin-releasing hormone receptorBinding affinity towards rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113936 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards rat pituitary Gonadotropin-releasing hormone receptorBinding affinity towards rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44432646 146689 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 146689 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44587395 172049 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 617 11 2 7 5.3 Cc1c(-c2cccc(OCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449373 172049 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 617 11 2 7 5.3 Cc1c(-c2cccc(OCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10394119 113936 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113936 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9809382 100195 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL292291 100195 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL216633 207579 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44449683 156759 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 9 2 7 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL407719 156759 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 9 2 7 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44577099 178155 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1021/jm701249f
CHEMBL468552 178155 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1021/jm701249f
9891852 95818 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL261145 95818 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
22716552 123240 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL362237 123240 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1016/j.bmcl.2005.01.009
9891852 10938 0 None 18 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117736 10938 0 None 18 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9891852 95818 0 None 13 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL261145 95818 0 None 13 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21045829 112886 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331855 112886 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9891852 95818 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmc.2007.09.026
CHEMBL261145 95818 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmc.2007.09.026
44352607 20435 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 607 11 0 9 5.5 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL130855 20435 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 607 11 0 9 5.5 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44352678 114722 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL334729 114722 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
10908122 183681 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1cccnc1 10.1021/jm0205402
CHEMBL48389 183681 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1cccnc1 10.1021/jm0205402
11027376 84791 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22563 84791 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11168330 98927 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
CHEMBL282707 98927 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
44353238 18336 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 553 10 0 7 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL127502 18336 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 553 10 0 7 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
11168330 98927 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL282707 98927 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
11027376 84791 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL22563 84791 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44451399 168144 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3cccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)c3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436906 168144 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3cccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)c3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL2370259 208066 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None None 10.1021/jm990432o
44309357 97624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 13 1 8 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL273358 97624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 13 1 8 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
44390780 63148 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 508 6 1 10 2.2 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccc3nsnc3c2)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL179953 63148 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 508 6 1 10 2.2 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccc3nsnc3c2)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
11455317 62544 0 None 851 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62544 0 None 851 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44576681 192858 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 553 11 2 6 4.9 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL526887 192858 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 553 11 2 6 4.9 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353271 22353 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 10 1 7 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL132616 22353 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 10 1 7 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44394767 125669 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL365001 125669 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44394894 168292 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 548 7 1 7 5.3 Cc1c(-c2csc(-c3ccc(F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL438201 168292 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 548 7 1 7 5.3 Cc1c(-c2csc(-c3ccc(F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9873729 11251 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 613 12 0 7 6.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117977 11251 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 613 12 0 7 6.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
86276161 109352 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 441 6 1 7 4.8 COc1nc(F)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
CHEMBL3233520 109352 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 441 6 1 7 4.8 COc1nc(F)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
21047858 9978 0 None 17 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115425 9978 0 None 17 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9828154 63523 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 523 10 0 9 2.1 COc1cccc(-n2c(=O)n(CCN(C)CCc3ccccn3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL180352 63523 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 523 10 0 9 2.1 COc1cccc(-n2c(=O)n(CCN(C)CCc3ccccn3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2004.11.026
44352747 21872 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 560 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132179 21872 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 560 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44267905 97899 0 None 13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275251 97899 0 None 13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44346348 113842 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 8 6.1 C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL333103 113842 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 8 6.1 C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
11477988 90565 0 None 954 2 Human 7.4 pKi = 7.4 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90565 0 None 954 2 Human 7.4 pKi = 7.4 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
11092567 101015 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 5.0 COCCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL297938 101015 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 5.0 COCCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11103551 101195 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 544 8 1 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCCC4)n3c2=O)c1 10.1021/jm0205402
CHEMBL299320 101195 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 544 8 1 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCCC4)n3c2=O)c1 10.1021/jm0205402
44340632 9415 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112188 9415 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44312806 11201 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
CHEMBL1179388 11201 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
CHEMBL73454 11201 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
44353247 115548 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL335610 115548 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
21047516 15158 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL121412 15158 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
44353247 115548 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.09.026
CHEMBL335610 115548 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.09.026
44353265 22110 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 644 17 2 7 6.0 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCN(CC)CC)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL132392 22110 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 644 17 2 7 6.0 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCN(CC)CC)n2c1=O 10.1016/s0960-894x(01)00780-6
21045834 16253 0 None -3 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL123301 16253 0 None -3 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11250647 1510 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 1510 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 1510 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 1510 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 1510 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44451406 96121 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 0 6 4.6 CC(CCN1CCc2c(c(=O)n(CCN3CCCCC3)c(=O)n2Cc2c(F)cccc2F)C1)CC(C)(C)C 10.1016/j.bmc.2007.09.026
CHEMBL263118 96121 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 0 6 4.6 CC(CCN1CCc2c(c(=O)n(CCN3CCCCC3)c(=O)n2Cc2c(F)cccc2F)C1)CC(C)(C)C 10.1016/j.bmc.2007.09.026
11282957 121806 0 None 1096 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121806 0 None 1096 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
44436018 146520 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 550 8 1 6 4.5 CN[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
CHEMBL392709 146520 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 550 8 1 6 4.5 CN[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
44353305 19609 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 10 0 8 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc([N+](=O)[O-])cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130195 19609 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 10 0 8 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc([N+](=O)[O-])cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL405918 210829 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
11261195 63360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL180124 63360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11261195 63360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL180124 63360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
11386605 89749 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23823 89749 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11786039 85340 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 540 9 0 6 5.0 Cc1c(-c2ccc3ccccc3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22937 85340 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 540 9 0 6 5.0 Cc1c(-c2ccc3ccccc3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11386605 89749 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23823 89749 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
44346649 113054 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 589 7 1 9 4.5 O=c1c2c(CN3CCNCC3)c(-c3ccc([N+](=O)[O-])cc3)sc2n(Cc2c(F)cccc2F)c(=O)n1-c1ccccc1 10.1016/s0960-894x(03)00746-7
CHEMBL332194 113054 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 589 7 1 9 4.5 O=c1c2c(CN3CCNCC3)c(-c3ccc([N+](=O)[O-])cc3)sc2n(Cc2c(F)cccc2F)c(=O)n1-c1ccccc1 10.1016/s0960-894x(03)00746-7
44389571 62804 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 471 6 1 6 4.1 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2)CC3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL178961 62804 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 471 6 1 6 4.1 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2)CC3)c1F 10.1016/j.bmcl.2005.01.009
44267903 161671 0 None -3 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL416337 161671 0 None -3 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44394779 66718 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3ccc(C(F)(F)F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL187243 66718 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3ccc(C(F)(F)F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44309559 102476 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL306431 102476 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
44309559 102476 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.09.026
CHEMBL306431 102476 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.09.026
44340656 109975 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL324759 109975 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340652 9349 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL111820 9349 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
11238459 89096 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 570 9 0 8 4.2 Cc1c(-c2ccc3c(c2)OC(F)(F)O3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23737 89096 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 570 9 0 8 4.2 Cc1c(-c2ccc3c(c2)OC(F)(F)O3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44432645 86760 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232752 86760 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44267906 166920 0 None -9 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL429949 166920 0 None -9 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
10983989 199978 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 9 1 7 3.6 Cc1c(-c2cccc(O)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL60618 199978 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 9 1 7 3.6 Cc1c(-c2cccc(O)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44451276 95582 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259878 95582 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11284264 84317 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 550 11 0 8 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1OC 10.1021/jm030472z
CHEMBL22300 84317 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 550 11 0 8 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1OC 10.1021/jm030472z
10907714 201462 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL64212 201462 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
11124671 201485 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 574 10 0 7 4.8 Cc1c(-c2cccc(OC(F)(F)F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL64273 201485 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 574 10 0 7 4.8 Cc1c(-c2cccc(OC(F)(F)F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44394608 66713 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL187217 66713 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44394841 165398 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 562 7 1 7 5.6 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1F 10.1016/j.bmcl.2004.07.022
CHEMBL425178 165398 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 562 7 1 7 5.6 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1F 10.1016/j.bmcl.2004.07.022
CHEMBL412504 211242 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCC(=O)NC[C@@H]2NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm990116+
11124921 191194 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 612 10 1 9 5.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1O 10.1021/jm0205402
CHEMBL51983 191194 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 612 10 1 9 5.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1O 10.1021/jm0205402
44436010 88918 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 4.8 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236967 88918 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 4.8 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44352957 116219 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 600 11 0 10 4.8 CCOC(=O)c1cn(Cc2ccccc2C#N)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL337433 116219 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 600 11 0 10 4.8 CCOC(=O)c1cn(Cc2ccccc2C#N)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11214860 84333 0 None -323 2 Rat 5.3 pKi = 5.3 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84333 0 None -323 2 Rat 5.3 pKi = 5.3 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
11191675 63037 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63037 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63037 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
44340637 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.07.022
CHEMBL112466 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.07.022
44340652 9349 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111820 9349 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
17757566 88100 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 10 0 7 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL235270 88100 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 10 0 7 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
17757565 146409 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 593 10 0 7 4.4 Cc1cc(Cl)ccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
CHEMBL392605 146409 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 593 10 0 7 4.4 Cc1cc(Cl)ccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
44387972 63530 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 514 7 1 8 2.8 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL180372 63530 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 514 7 1 8 2.8 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
11214294 121668 0 None 912 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121668 0 None 912 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44340749 108618 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL321376 108618 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
9829468 188171 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL50546 188171 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44340749 108618 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL321376 108618 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
9829468 188171 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm701249f
CHEMBL50546 188171 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm701249f
CHEMBL2371542 208324 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44434414 88084 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
CHEMBL235179 88084 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
44267906 166920 0 None 9 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL429949 166920 0 None 9 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44399944 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL191817 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44399944 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44399944 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL191817 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL191817 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44399944 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL191817 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44340637 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340637 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL112466 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1021/jm701249f
44340637 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL112466 9473 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2005.01.009
11156980 62249 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL178281 62249 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
11374717 121768 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359810 121768 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL419270 121768 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44399944 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL191817 68278 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432639 86521 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL232356 86521 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
44267887 98016 0 None -41 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 98016 0 None -41 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL414275 211361 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44353249 167870 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 659 17 1 8 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCN(CC)CC)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434995 167870 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 659 17 1 8 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCN(CC)CC)cc1 10.1016/s0960-894x(01)00780-6
10051739 84994 0 None 501 2 Human 7.3 pKi = 7.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 84994 0 None 501 2 Human 7.3 pKi = 7.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44451350 95696 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 544 8 1 6 4.5 CNC(Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C)cc1C)C2)c1ccccc1 10.1016/j.bmc.2007.09.026
CHEMBL260552 95696 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 544 8 1 6 4.5 CNC(Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C)cc1C)C2)c1ccccc1 10.1016/j.bmc.2007.09.026
9939030 155175 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 623 11 1 6 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2cc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)cc2c1=O 10.1016/j.bmc.2007.09.026
CHEMBL405449 155175 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 623 11 1 6 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2cc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)cc2c1=O 10.1016/j.bmc.2007.09.026
44267882 166020 0 None 12 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL428008 166020 0 None 12 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
14557580 88926 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 972 26 11 11 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369785 88926 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 972 26 11 11 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00130a019
9916573 156501 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 593 11 0 9 5.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL407399 156501 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 593 11 0 9 5.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44394578 129636 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 586 7 1 7 6.4 Cc1c(-c2csc(-c3ccc(C(C)(C)C)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367806 129636 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 586 7 1 7 6.4 Cc1c(-c2csc(-c3ccc(C(C)(C)C)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11752557 63353 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
CHEMBL180117 63353 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
CHEMBL74925 63353 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
44451498 155069 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1700 30 7 19 9.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC(C(=O)NCC#Cc3ccccc3C#CCNC(=O)C3CCN(C(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)CC3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL404611 155069 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1700 30 7 19 9.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC(C(=O)NCC#Cc3ccccc3C#CCNC(=O)C3CCN(C(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)CC3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL2370249 208060 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
11202795 112322 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL330804 112322 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
11477970 89055 0 None 281 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL23729 89055 0 None 281 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm049791w
11202795 112322 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL330804 112322 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
21046387 110150 0 None 53 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL325843 110150 0 None 53 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44267875 15379 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12204 15379 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44451391 168287 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)cc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL438168 168287 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)cc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21046569 11888 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 9 2 7 7.0 COC(=O)c1cc(C)nc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL118330 11888 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 9 2 7 7.0 COC(=O)c1cc(C)nc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
21045818 112584 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331337 112584 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11050500 101365 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 636 9 0 8 6.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCC(c2ccccc2)CC1 10.1021/jm0205402
CHEMBL300484 101365 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 636 9 0 8 6.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCC(c2ccccc2)CC1 10.1021/jm0205402
44435828 88663 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 11 1 7 4.0 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(CCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2007.05.029
CHEMBL236546 88663 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 11 1 7 4.0 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(CCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2007.05.029
44309631 102123 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 652 14 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2cccnc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL304156 102123 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 652 14 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2cccnc2)cc1 10.1016/s0960-894x(02)00370-0
44587397 171777 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 589 9 2 7 4.5 Cc1c(-c2cccc(OCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL447592 171777 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 589 9 2 7 4.5 Cc1c(-c2cccc(OCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
9891852 95818 0 None -13 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL261145 95818 0 None -13 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44436000 146657 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.3 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C4CCCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392815 146657 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.3 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C4CCCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
21045831 10380 0 None -7 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116611 10380 0 None -7 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047815 14764 0 None -30 2 Rat 5.3 pKi = 5.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120834 14764 0 None -30 2 Rat 5.3 pKi = 5.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340646 9582 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113059 9582 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11421385 167846 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
CHEMBL433302 167846 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
CHEMBL434906 167846 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
11049737 101879 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 532 8 0 7 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCCC3c3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL303811 101879 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 532 8 0 7 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCCC3c3ccccn3)c2=O)c1 10.1021/jm034041s
44451345 96050 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262599 96050 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451474 168181 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL437260 168181 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21048462 109815 0 None 60 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323863 109815 0 None 60 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44433200 149639 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 555 7 0 8 4.1 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccc(-n4ccnc4)cc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL395183 149639 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 555 7 0 8 4.1 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccc(-n4ccnc4)cc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL415608 211437 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44343931 109899 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL324375 109899 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
9910626 10275 0 None 1 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
CHEMBL116246 10275 0 None 1 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
44343931 109899 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL324375 109899 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44400195 69030 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL193089 69030 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
21047519 14286 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
CHEMBL120048 14286 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
44340697 110167 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325942 110167 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340612 9472 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112461 9472 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
11477970 89055 0 None 281 2 Human 6.3 pKi = 6.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89055 0 None 281 2 Human 6.3 pKi = 6.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44309359 101843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 619 10 1 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(S)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL303621 101843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 619 10 1 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(S)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
9910626 10275 0 None -1 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
CHEMBL116246 10275 0 None -1 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
44347048 14329 0 None -18 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120164 14329 0 None -18 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9911446 10666 0 None -33 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117170 10666 0 None -33 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267864 167184 0 None -30 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
CHEMBL430312 167184 0 None -30 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
44267905 97899 0 None -13 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275251 97899 0 None -13 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11421385 167846 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL433302 167846 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL434906 167846 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
44347005 113953 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333461 113953 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11752557 63353 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
CHEMBL180117 63353 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
CHEMBL74925 63353 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
44399956 123514 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL363094 123514 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44346239 14327 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 707 12 2 8 7.2 CC(C)C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL120149 14327 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 707 12 2 8 7.2 CC(C)C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44434436 150428 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395825 150428 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44577100 177907 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 452 6 1 6 3.1 N[C@@H](Cn1c(=O)c(Cc2c(F)cccc2F)nn(-c2ccccc2F)c1=O)c1ccccc1 10.1021/jm701249f
CHEMBL466541 177907 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 452 6 1 6 3.1 N[C@@H](Cn1c(=O)c(Cc2c(F)cccc2F)nn(-c2ccccc2F)c1=O)c1ccccc1 10.1021/jm701249f
44451356 95903 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL261649 95903 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44387909 122239 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 495 8 1 9 2.0 COc1cccc(-n2c(=O)n(CCC(N)c3cccnc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL360472 122239 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 495 8 1 9 2.0 COc1cccc(-n2c(=O)n(CCC(N)c3cccnc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
9960268 188390 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 596 10 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1 10.1021/jm0205402
CHEMBL50856 188390 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 596 10 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1 10.1021/jm0205402
44340844 110051 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL325233 110051 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11751752 13436 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049791w
CHEMBL119391 13436 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049791w
11374717 121768 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL359810 121768 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL419270 121768 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
44400230 68327 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL192172 68327 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
1179 945 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 945 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 945 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
44400230 68327 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL192172 68327 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11374717 121768 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL359810 121768 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL419270 121768 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
1179 945 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 945 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 945 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
21045805 13657 0 None 5 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL119546 13657 0 None 5 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44215933 95619 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3nccs3)c2=O)c1F 10.1016/j.bmc.2007.09.026
CHEMBL260062 95619 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3nccs3)c2=O)c1F 10.1016/j.bmc.2007.09.026
44432655 148942 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394634 148942 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44400354 132970 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 559 8 1 6 5.5 CC(C)Oc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL370711 132970 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 559 8 1 6 5.5 CC(C)Oc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44267865 160825 0 None 10 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
CHEMBL412634 160825 0 None 10 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
11236870 10928 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL117670 10928 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
11294792 62943 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62943 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
10345138 122029 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122029 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122029 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
11236870 10928 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL117670 10928 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
11226753 62999 0 None 389 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 62999 0 None 389 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11180219 110720 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110720 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11180219 110720 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL326504 110720 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
9823968 109979 0 None 1 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
CHEMBL324771 109979 0 None 1 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
1184 3663 31 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
9874838 3663 31 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL71917 3663 31 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
11751752 13436 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049218c
CHEMBL119391 13436 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049218c
44436011 88053 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 9 0 7 4.9 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(CCc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL235046 88053 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 9 0 7 4.9 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(CCc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44451447 156121 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406960 156121 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352949 115568 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL335650 115568 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11444384 63074 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
CHEMBL179663 63074 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
CHEMBL311380 63074 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
44449120 94776 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94776 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44346666 112327 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 9 0 7 6.9 CN(Cc1ccccc1)Cc1c(-c2ccc(N(C)C)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL330835 112327 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 9 0 7 6.9 CN(Cc1ccccc1)Cc1c(-c2ccc(N(C)C)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
9958318 89782 0 None 15 2 Human 6.2 pKi = 6.2 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89782 0 None 15 2 Human 6.2 pKi = 6.2 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
11167850 2691 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 2691 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 2691 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 2691 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL216930 207591 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44353231 116296 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 595 12 0 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL337865 116296 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 595 12 0 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44451420 95753 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260812 95753 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44387883 62929 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 478 8 1 8 2.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)CC(C)C)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL179212 62929 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 478 8 1 8 2.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)CC(C)C)c2=O)c1F 10.1016/j.bmcl.2005.05.038
11341990 62156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
CHEMBL178127 62156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
CHEMBL76277 62156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
21047807 112474 0 None 23 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331087 112474 0 None 23 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44353284 167813 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 652 15 2 8 5.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCOC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434621 167813 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 652 15 2 8 5.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCOC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44388009 128149 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 7 1 8 2.9 COc1cccc(-n2c(=O)n(C[C@H](N)c3ccccc3)c(=O)n(C(C)c3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL366883 128149 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 7 1 8 2.9 COc1cccc(-n2c(=O)n(C[C@H](N)c3ccccc3)c(=O)n(C(C)c3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267882 166020 0 None -12 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL428008 166020 0 None -12 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11238091 62162 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
CHEMBL178142 62162 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
CHEMBL311407 62162 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
44353263 22033 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 634 10 0 9 6.9 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(-c3nc(C(C)(C)C)co3)c(=O)n12 10.1016/s0960-894x(01)00780-6
CHEMBL132338 22033 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 634 10 0 9 6.9 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(-c3nc(C(C)(C)C)co3)c(=O)n12 10.1016/s0960-894x(01)00780-6
44346594 15383 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 548 7 0 8 5.2 CN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL122064 15383 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 548 7 0 8 5.2 CN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44295109 101198 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 530 8 1 6 6.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCC4)n3c2=O)c1 10.1021/jm0205402
CHEMBL299335 101198 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 530 8 1 6 6.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCC4)n3c2=O)c1 10.1021/jm0205402
11477988 90565 0 None -954 2 Rat 5.2 pKi = 5.2 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90565 0 None -954 2 Rat 5.2 pKi = 5.2 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
11294792 62943 0 None 380 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62943 0 None 380 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44309652 202592 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccccc4OC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL71400 202592 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccccc4OC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
11192019 13134 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human gonadotropin-releasing hormone receptorBinding affinity for human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL119149 13134 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human gonadotropin-releasing hormone receptorBinding affinity for human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
44576678 170471 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 11 1 7 5.8 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL445691 170471 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 11 1 7 5.8 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11192019 13134 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL119149 13134 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
44387888 60147 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3cccc(F)c3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175491 60147 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3cccc(F)c3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44388033 61418 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 497 7 1 9 2.1 COc1cccc(-n2c(=O)n(Cc3cccnc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL177182 61418 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 497 7 1 9 2.1 COc1cccc(-n2c(=O)n(Cc3cccnc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21045823 113630 0 None 40 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL332923 113630 0 None 40 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267865 160825 0 None -10 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
CHEMBL412634 160825 0 None -10 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
44400122 132827 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 2 6 3.5 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL370480 132827 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 2 6 3.5 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44432637 154421 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 492 8 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401225 154421 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 492 8 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
44352641 117647 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 605 12 0 10 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340856 117647 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 605 12 0 10 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL263690 208831 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CC(=O)NC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
11444384 63074 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
CHEMBL179663 63074 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
CHEMBL311380 63074 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
44309404 102263 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 648 10 0 8 6.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2F)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL305034 102263 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 648 10 0 8 6.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2F)cc1 10.1016/s0960-894x(02)00371-2
21045817 114039 0 None 22 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333730 114039 0 None 22 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44448860 94608 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL255242 94608 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
11295556 98780 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.3 CCOc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL281776 98780 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.3 CCOc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44576642 187201 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 513 7 2 6 4.1 N[C@@H](Cn1c(=O)c(-c2ccc(CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL495882 187201 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 513 7 2 6 4.1 N[C@@H](Cn1c(=O)c(-c2ccc(CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44434437 150429 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395826 150429 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44267863 98053 0 None -2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL276217 98053 0 None -2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11353175 99007 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 537 9 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283170 99007 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 537 9 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1F 10.1021/jm030472z
44394616 66011 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 617 9 2 9 5.7 CCOC(=O)Nc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL185143 66011 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 617 9 2 9 5.7 CCOC(=O)Nc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
21047618 114019 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333574 114019 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44288082 162606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 981 10 1 14 8.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL418067 162606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 981 10 1 14 8.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44449153 154525 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL401807 154525 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
10439419 101700 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL302769 101700 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
10439419 101700 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm701249f
CHEMBL302769 101700 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm701249f
11477615 121617 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 503 9 0 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CC(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL359682 121617 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 503 9 0 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CC(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
10439419 101700 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL302769 101700 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44587394 171896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL448253 171896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
21047583 15113 0 None 10 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121367 15113 0 None 10 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44288073 168849 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 965 12 2 14 7.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL442482 168849 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 965 12 2 14 7.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
25156669 188531 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 13 2 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL510538 188531 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 13 2 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44400121 126883 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL365985 126883 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44400121 126883 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL365985 126883 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11050145 192754 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 581 10 0 7 6.4 CCN(CCc1ccccn1)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL52506 192754 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 581 10 0 7 6.4 CCN(CCc1ccccn1)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11387100 10126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL116074 10126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11387100 10126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116074 10126 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049791w
44267866 96652 0 None 4 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL267568 96652 0 None 4 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11179922 86878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
CHEMBL23321 86878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
44394896 65958 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 545 8 2 8 5.2 Cc1c(-c2csc(Nc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL184855 65958 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 545 8 2 8 5.2 Cc1c(-c2csc(Nc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11179922 86878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23321 86878 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
44436019 167077 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 4.9 CN(C)[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
CHEMBL430171 167077 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 4.9 CN(C)[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
44387945 122188 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL360447 122188 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
11157017 121861 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
CHEMBL360056 121861 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
CHEMBL72199 121861 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
20728209 122794 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 443 5 1 6 3.5 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL361619 122794 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 443 5 1 6 3.5 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44451294 95657 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1647 38 8 18 11.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260318 95657 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1647 38 8 18 11.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21045831 10380 0 None 7 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116611 10380 0 None 7 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL2370251 208061 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL329695 209563 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
44340860 9509 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112625 9509 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11363829 10065 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL115965 10065 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)(C)C)c2=O)c1F 10.1021/jm049791w
25156399 188451 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 603 10 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509440 188451 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 603 10 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
9915597 183598 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 552 8 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL48316 183598 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 552 8 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccc4)n3c2=O)c1 10.1021/jm0205402
44340840 112812 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1ccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)cc1 10.1016/s0960-894x(03)00619-x
CHEMBL331592 112812 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1ccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)cc1 10.1016/s0960-894x(03)00619-x
CHEMBL405420 210802 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44451486 157620 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)cc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL408760 157620 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)cc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44388026 129283 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 521 7 1 9 2.6 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL367548 129283 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 521 7 1 9 2.6 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047858 9978 0 None -17 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115425 9978 0 None -17 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9891852 10938 0 None -18 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117736 10938 0 None -18 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
10439527 168902 0 None -288 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL443027 168902 0 None -288 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11214294 121668 0 None 912 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121668 0 None 912 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
21045828 14380 0 None -2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120420 14380 0 None -2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44451408 95736 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260750 95736 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11214295 86548 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL23237 86548 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
11214295 86548 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23237 86548 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11341990 62156 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
CHEMBL178127 62156 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
CHEMBL76277 62156 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
44387898 60704 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 508 8 1 8 2.9 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL176284 60704 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 508 8 1 8 2.9 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
10051739 84994 0 None -501 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 84994 0 None -501 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44346662 113914 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 633 12 0 9 5.9 CCN(CC)CCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333213 113914 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 633 12 0 9 5.9 CCN(CC)CCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44352652 116968 0 None -245 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL339968 116968 0 None -245 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11282957 121806 0 None -1096 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121806 0 None -1096 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
9983568 98512 0 None -263 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98512 0 None -263 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44576655 187628 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 9 2 8 3.6 NCC(=O)OCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL499307 187628 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 9 2 8 3.6 NCC(=O)OCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
11238091 62162 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
CHEMBL178142 62162 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
CHEMBL311407 62162 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
44451379 168403 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL439076 168403 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352665 117758 0 None -43 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340934 117758 0 None -43 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
10875519 188714 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 575 8 0 9 3.9 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCN(C)CC1 10.1021/jm0205402
CHEMBL51232 188714 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 575 8 0 9 3.9 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCN(C)CC1 10.1021/jm0205402
11294792 62943 0 None -380 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62943 0 None -380 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
11455176 98589 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL280430 98589 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11455176 98589 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL280430 98589 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
44341074 9835 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114619 9835 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
21045807 16123 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 8 2 5 7.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(C(F)(F)F)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL122653 16123 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 8 2 5 7.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(C(F)(F)F)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11226171 87008 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23337 87008 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11226171 87008 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23337 87008 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
44309617 202250 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 605 10 0 7 6.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL69361 202250 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 605 10 0 7 6.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
21047937 110796 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326606 110796 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44288079 99737 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 896 11 3 14 5.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](NC)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL288396 99737 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 896 11 3 14 5.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](NC)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267870 97656 0 None -8 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273536 97656 0 None -8 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11421518 164733 0 None -1047 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164733 0 None -1047 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44267904 97951 0 None -6 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275521 97951 0 None -6 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11103767 101311 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 569 10 1 8 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CO)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL300079 101311 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 569 10 1 8 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CO)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44400188 69022 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 501 6 1 5 4.7 N[C@@H](Cn1c(=O)c(-c2ccccc2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL193031 69022 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 501 6 1 5 4.7 N[C@@H](Cn1c(=O)c(-c2ccccc2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44347047 16407 0 None -5 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL124056 16407 0 None -5 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9984259 109999 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
CHEMBL324912 109999 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
9984259 109999 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 109999 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
9984259 109999 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 109999 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44400353 68317 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 599 8 1 6 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCC(F)(F)F)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL192096 68317 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 599 8 1 6 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCC(F)(F)F)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11307227 122524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 6 5.8 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL360935 122524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 6 5.8 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL2371513 208309 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H]1CCC(=O)NCCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44267870 97656 0 None 8 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273536 97656 0 None 8 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44309319 202010 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 609 12 1 8 5.9 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL67638 202010 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 609 12 1 8 5.9 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
44435992 96047 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 597 10 0 8 4.8 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262581 96047 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 597 10 0 8 4.8 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
21047583 15113 0 None -10 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121367 15113 0 None -10 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352679 114989 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL335196 114989 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44387920 63538 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3F)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL180421 63538 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3F)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL2370261 208067 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL329946 209567 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44435981 146404 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 623 11 0 9 2.9 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392603 146404 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 623 11 0 9 2.9 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2007.05.029
44340641 110075 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 529 13 1 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325391 110075 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 529 13 1 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
11260704 98209 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2ccccc2F)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL277439 98209 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2ccccc2F)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44451446 168140 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436862 168140 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11249548 98620 0 None 97 2 Human 6.1 pKi = 6.1 Binding
In vivo inhibition of monkey Gonadotropin releasing hormone receptorIn vivo inhibition of monkey Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98620 0 None 97 2 Human 6.1 pKi = 6.1 Binding
In vivo inhibition of monkey Gonadotropin releasing hormone receptorIn vivo inhibition of monkey Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
44387922 60207 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccc(F)cc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175869 60207 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccc(F)cc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
9823968 109979 0 None -1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
CHEMBL324771 109979 0 None -1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
21046570 112575 0 None -34 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL331277 112575 0 None -34 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44340643 110843 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 8 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(CCc4ccccn4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL326885 110843 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 8 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(CCc4ccccn4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44451343 96006 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1591 34 8 18 9.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262335 96006 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1591 34 8 18 9.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44340824 9366 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3cccc(F)c3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111933 9366 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3cccc(F)c3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435984 88338 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
CHEMBL236332 88338 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
44435983 88337 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1cccc(Cl)c1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236331 88337 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1cccc(Cl)c1)C2 10.1016/j.bmc.2007.05.029
44451258 166861 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1729 32 8 20 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL429690 166861 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1729 32 8 20 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352942 22396 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 609 11 0 9 5.6 CCOC(=O)c1cn(Cc2ccccc2Cl)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132661 22396 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 609 11 0 9 5.6 CCOC(=O)c1cn(Cc2ccccc2Cl)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44388018 60137 0 None 389 2 Human 7.1 pKi = 7.1 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60137 0 None 389 2 Human 7.1 pKi = 7.1 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047784 110135 0 None -36 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL325747 110135 0 None -36 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11191675 63037 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63037 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63037 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
11226531 99046 0 None 169 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99046 0 None 169 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44389647 64228 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 455 6 1 7 3.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1 10.1016/j.bmcl.2005.01.009
CHEMBL181582 64228 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 455 6 1 7 3.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1 10.1016/j.bmcl.2005.01.009
44346665 112326 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 10 1 7 7.7 CC(C)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL330834 112326 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 10 1 7 7.7 CC(C)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
11284357 60677 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
CHEMBL176270 60677 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
CHEMBL72913 60677 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
11329628 62680 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL178805 62680 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL73575 62680 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL405837 210827 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44390758 64600 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 468 6 1 7 2.3 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL182284 64600 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 468 6 1 7 2.3 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
44340652 9349 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL111820 9349 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21047631 10843 0 None -5 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117330 10843 0 None -5 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44352657 21336 0 None -269 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
CHEMBL131665 21336 0 None -269 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
44387896 129139 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL367388 129139 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44394778 125353 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 8 1 7 5.1 Cc1c(-c2csc(Cc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL364842 125353 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 8 1 7 5.1 Cc1c(-c2csc(Cc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9852184 10574 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 628 13 0 8 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117069 10574 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 628 13 0 8 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44346396 112860 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 625 9 0 9 6.1 CN(Cc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL331762 112860 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 625 9 0 9 6.1 CN(Cc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44387896 129139 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL367388 129139 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44347005 113953 0 None 6 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333461 113953 0 None 6 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44400247 121515 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 571 10 2 9 2.5 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)CCO)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL359558 121515 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 571 10 2 9 2.5 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)CCO)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44353288 167783 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 662 13 2 7 6.4 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434423 167783 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 662 13 2 7 6.4 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44587403 188230 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 647 13 2 8 4.8 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL506338 188230 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 647 13 2 8 4.8 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
10394119 113936 0 None -1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113936 0 None -1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL438712 212029 0 None - 1 Rat 8.0 pKi = 8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44340623 9374 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111980 9374 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
21047633 163911 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL421418 163911 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44343881 10862 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 603 12 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117346 10862 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 603 12 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
11082604 101276 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 608 8 0 8 5.7 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCc2ccccc2C1 10.1021/jm0205402
CHEMBL299850 101276 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 608 8 0 8 5.7 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCc2ccccc2C1 10.1021/jm0205402
22716607 64433 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 493 5 1 6 4.9 NC(Cn1c(=O)c(-c2ccccc2Cl)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL181945 64433 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 493 5 1 6 4.9 NC(Cn1c(=O)c(-c2ccccc2Cl)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44451419 96487 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL266172 96487 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451430 155361 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406084 155361 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047633 163911 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL421418 163911 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11431754 13172 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL119185 13172 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
44387961 165457 0 None -144 2 Rat 5.0 pKi = 5.0 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165457 0 None -144 2 Rat 5.0 pKi = 5.0 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44436001 161121 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.6 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccc4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL413239 161121 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.6 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccc4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44309671 202150 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 554 10 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL68664 202150 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 554 10 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
44340642 9563 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112881 9563 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309388 102060 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 609 7 0 9 5.2 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCCN(C)CC2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304067 102060 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 609 7 0 9 5.2 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCCN(C)CC2)cc1 10.1016/s0960-894x(02)00371-2
44340688 9503 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 0 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112611 9503 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 0 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11489334 10378 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CCc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL116576 10378 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CCc3ccccc3)c2=O)c1F 10.1021/jm049791w
11294949 13912 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL119739 13912 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
44435818 88662 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 399 4 1 6 2.0 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CNCC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236545 88662 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 399 4 1 6 2.0 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CNCC3)c1 10.1016/j.bmc.2007.05.029
11294949 13912 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL119739 13912 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
44587400 172592 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 13 2 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL452198 172592 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 13 2 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11157017 121861 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
CHEMBL360056 121861 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
CHEMBL72199 121861 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
44435822 153645 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 519 7 0 7 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2OC)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL398583 153645 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 519 7 0 7 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2OC)CC3)c1 10.1016/j.bmc.2007.05.029
44435825 88062 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 545 10 0 7 3.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccccc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235084 88062 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 545 10 0 7 3.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccccc1)C2 10.1016/j.bmc.2007.05.029
11455317 62544 0 None -851 2 Rat 5.0 pKi = 5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62544 0 None -851 2 Rat 5.0 pKi = 5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11980076 206701 27 None - 1 Human 8.1 pIC50 = 8.1 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 206701 27 None - 1 Human 8.1 pIC50 = 8.1 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
1175 2256 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
1559 2256 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
657181 2256 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
CHEMBL1201199 2256 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
DB00007 2256 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
3823 49936 38 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 49936 38 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 49936 38 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
25077405 2665 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
3902 2665 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201309 2665 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00666 2665 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
1162 1793 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 1793 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3878 1795 0 None - 1 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17254668
188304 1594 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 1594 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 1594 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 323 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 323 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 323 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 1895 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
25077495 1358 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 1358 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 1358 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 1358 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 731 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11167850 2691 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
1178 2691 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
1187 2691 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
CHEMBL179691 2691 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
11250647 1510 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
5293 1510 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
8362 1510 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
CHEMBL1208155 1510 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
DB11979 1510 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
101755083 1327 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
16136245 1327 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
4379 1327 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
5585 1327 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL415606 1327 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB06699 1327 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
1190 867 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
25074887 867 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
583 867 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
CHEMBL1200490 867 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
DB00050 867 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
1177 3794 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
25074470 3794 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
2968 3794 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201334 3794 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB06825 3794 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
1188 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
16131215 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
35 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1252 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00106 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
11225 1093 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.
Guide to Pharmacology 645 10 0 6 6.0 FCCOc1cccc(c1F)c1c(C)n(Cc2c(F)cccc2C(F)(F)F)c(=O)n(c1=O)C[C@H](N1CCCC1=O)c1ccccc1 32677155
154699464 1093 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.
Guide to Pharmacology 645 10 0 6 6.0 FCCOc1cccc(c1F)c1c(C)n(Cc2c(F)cccc2C(F)(F)F)c(=O)n(c1=O)C[C@H](N1CCCC1=O)c1ccccc1 32677155
1162 1793 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 1793 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 1793 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 1793 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16132914 1793 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 1793 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1162 1793 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 1793 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
101755083 1327 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
16136245 1327 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
4379 1327 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
5585 1327 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
CHEMBL415606 1327 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
DB06699 1327 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
1175 2256 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1559 2256 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
657181 2256 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1201199 2256 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00007 2256 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
11250647 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
11250647 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
5293 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
5293 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
8362 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
8362 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
CHEMBL1208155 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
CHEMBL1208155 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
DB11979 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
DB11979 1510 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
188304 1594 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 1594 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 1594 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 323 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 323 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 323 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 1895 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1188 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16131215 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
35 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1252 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00106 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1177 3794 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 3794 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 3794 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 3794 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 3794 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
101827019 2066 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
16130938 2066 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
3854 2066 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
73952264 2066 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
CHEMBL3989438 2066 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
25077495 1358 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 1358 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 1358 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 1358 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1190 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1190 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
1190 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
25074887 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
25074887 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
25074887 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
583 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
583 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
583 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
CHEMBL1200490 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1200490 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
CHEMBL1200490 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
DB00050 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00050 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
DB00050 867 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
3860 731 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 731 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 731 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 731 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 731 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1180 1271 0 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1185 3632 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
3038517 3632 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
CHEMBL22055 3632 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
DB06494 3632 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
1191 1257 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1170 1892 0 None - 1 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1179 945 31 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
9957278 945 31 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
CHEMBL494803 945 31 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
10279142 1589 0 None - 1 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1182 1589 0 None - 1 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1181 1272 0 None - 1 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1177 3794 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 3794 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 3794 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 3794 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 3794 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
11167850 2691 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1178 2691 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1187 2691 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
CHEMBL179691 2691 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
11167850 2691 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1178 2691 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1187 2691 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
CHEMBL179691 2691 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1189 423 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
16132443 423 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077