Ligand source activities (1 row/activity)





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
44570962 183265 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480821 183265 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
145950336 162265 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 3 3 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4172656 162265 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 3 3 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
156016416 177073 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641513 177073 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
16752684 94050 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251572 94050 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156014430 176639 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4635542 176639 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
156016416 177073 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641513 177073 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
16752684 94050 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2008.12.042
CHEMBL251572 94050 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2008.12.042
44570963 183288 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481013 183288 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
156014430 176639 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4635542 176639 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
44444563 154404 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)cc1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL401134 154404 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)cc1)CC2 10.1016/j.bmcl.2007.09.067
156011926 176816 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4638297 176816 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44571002 190494 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H](O)[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL518774 190494 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H](O)[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
44449987 95436 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 16 4 10 0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCSCCO 10.1016/j.bmcl.2008.03.059
CHEMBL259166 95436 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 16 4 10 0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCSCCO 10.1016/j.bmcl.2008.03.059
25010378 158839 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 525 16 4 11 -0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(=O)(=O)CCO 10.1016/j.bmcl.2008.03.059
CHEMBL410074 158839 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 525 16 4 11 -0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(=O)(=O)CCO 10.1016/j.bmcl.2008.03.059
44449955 158853 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 509 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
CHEMBL410085 158853 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 509 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
156011926 176816 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4638297 176816 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
156017918 177222 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4643530 177222 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
156015100 176988 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640507 176988 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
156017918 177222 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4643530 177222 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
44570960 183396 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 417 4 1 5 2.4 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481796 183396 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 417 4 1 5 2.4 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
24894012 176213 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 497 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
CHEMBL460680 176213 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 497 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
156015100 176988 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640507 176988 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44437979 10214 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162065 10214 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
44437979 10214 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162065 10214 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
44454303 97107 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL270666 97107 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
156020725 177521 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647963 177521 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44570764 183457 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 481 4 1 4 3.8 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(Cl)ccc3Cl)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL482220 183457 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 481 4 1 4 3.8 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(Cl)ccc3Cl)cc2)C1 10.1016/j.bmcl.2008.12.042
24803512 88565 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364468 88565 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1Cl 10.6019/CHEMBL2364335
156020725 177521 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647963 177521 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
9917957 109217 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Compound was evaluated for GH release for effect on human GH secretagogue receptorCompound was evaluated for GH release for effect on human GH secretagogue receptor
ChEMBL 683 14 4 5 4.3 NC(=O)CN(CCc1ccccc1)C(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1021/jm970342o
CHEMBL322912 109217 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Compound was evaluated for GH release for effect on human GH secretagogue receptorCompound was evaluated for GH release for effect on human GH secretagogue receptor
ChEMBL 683 14 4 5 4.3 NC(=O)CN(CCc1ccccc1)C(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1021/jm970342o
44447855 193177 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 539 15 4 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL539929 193177 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 539 15 4 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
178024 1932 30 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1932 30 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1932 30 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
156013414 176888 4 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4639111 176888 4 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156013297 176900 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639229 176900 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44452749 95755 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 7 2 6 4.5 COc1ccc(F)c(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL260819 95755 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 7 2 6 4.5 COc1ccc(F)c(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
44570765 190834 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL519301 190834 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
59007047 88523 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364427 88523 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1C 10.6019/CHEMBL2364335
178024 1932 30 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1932 30 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1932 30 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
25022640 97339 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL271876 97339 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454337 155051 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL404545 155051 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44447839 94537 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 499 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254765 94537 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 499 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156013414 176888 4 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4639111 176888 4 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156013297 176900 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639229 176900 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44447857 166312 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL428592 166312 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156019724 177407 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646219 177407 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
22888474 63119 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL179823 63119 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
11306502 63296 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63296 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11306502 63296 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63296 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11306502 63296 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63296 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888476 122290 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL360547 122290 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
22888476 122290 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL360547 122290 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
44454117 155004 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155004 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
44444559 93987 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 451 4 1 5 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251169 93987 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 451 4 1 5 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
156011750 176706 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636502 176706 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156019724 177407 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646219 177407 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
44453123 97524 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 503 6 2 5 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(Cl)ccc2F)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL272753 97524 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 503 6 2 5 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(Cl)ccc2F)cc1 10.1016/j.bmcl.2007.12.021
44570966 182977 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480037 182977 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
59007062 88525 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364429 88525 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1F 10.6019/CHEMBL2364335
24803514 88570 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364472 88570 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1Cl 10.6019/CHEMBL2364335
44447852 155010 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 477 14 4 10 0.6 Cc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL404354 155010 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 477 14 4 10 0.6 Cc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156011750 176706 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636502 176706 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
44450016 160001 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 17 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411259 160001 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 17 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCCO 10.1016/j.bmcl.2008.03.059
44454367 94804 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 94804 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
22867441 10203 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161835 10203 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
16114096 78735 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113324 78735 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
22867441 10203 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161835 10203 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
44447841 154527 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL401827 154527 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
69195371 88449 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364354 88449 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44450101 158901 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 13 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
CHEMBL410135 158901 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 13 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
44391039 131253 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 540 9 1 7 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL369329 131253 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 540 9 1 7 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44449988 160542 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 477 16 4 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCOCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411697 160542 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 477 16 4 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCOCCO 10.1016/j.bmcl.2008.03.059
44447843 94565 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C(F)(F)F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254973 94565 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C(F)(F)F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
10280020 62747 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 529 8 1 5 6.2 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(Cl)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178900 62747 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 529 8 1 5 6.2 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(Cl)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
156021297 177505 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 177505 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44444571 93532 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248544 93532 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
10553921 104068 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL310457 104068 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
10345516 138732 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
CHEMBL379074 138732 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
156012122 176797 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 176797 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021297 177505 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 177505 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11584048 97566 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1Cl 10.1016/j.bmcl.2007.12.021
CHEMBL272993 97566 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1Cl 10.1016/j.bmcl.2007.12.021
24755624 156746 1 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL407706 156746 1 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2007.12.021
24755624 156746 1 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2008.12.042
CHEMBL407706 156746 1 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2008.12.042
69197353 88503 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364408 88503 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44454060 154781 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 154781 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
10553921 104068 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL310457 104068 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
10345516 138732 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
CHEMBL379074 138732 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
127047525 139224 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798559 139224 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
156022162 177622 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4649634 177622 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156012122 176797 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 176797 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
20600693 63111 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 566 11 1 6 4.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL179785 63111 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 566 11 1 6 4.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44560945 178513 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 391 9 2 7 2.1 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
CHEMBL471751 178513 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 391 9 2 7 2.1 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
216208 9620 27 None -5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9620 27 None -5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
44449891 96014 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL262358 96014 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
216208 9620 27 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9620 27 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
156021478 177471 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647258 177471 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
44437955 10212 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162063 10212 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
9807597 182425 3 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL47938 182425 3 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
156018364 177329 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177329 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021478 177471 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647258 177471 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
156022090 177619 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4649603 177619 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156022162 177622 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4649634 177622 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
56926175 68656 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923504 68656 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926356 68662 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
CHEMBL1923512 68662 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
56926461 68679 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923609 68679 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926462 68680 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923610 68680 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
57399248 68687 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923617 68687 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
11664206 68696 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923626 68696 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926894 68707 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923638 68707 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
11526745 68711 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923642 68711 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11526696 71243 13 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923502 71243 13 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1963249 71243 13 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
134130631 141829 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
CHEMBL3889512 141829 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
134137202 142282 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3893048 142282 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134137257 142593 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3895776 142593 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134133518 142909 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3898348 142909 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134133352 142961 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3898794 142961 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
134134286 143150 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3900284 143150 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134135712 143594 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
CHEMBL3903845 143594 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
11512561 143824 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3905791 143824 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134133037 144022 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3907497 144022 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
134132893 144318 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3909834 144318 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134132152 144387 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3910300 144387 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
134142218 144742 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3913052 144742 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
134142433 144781 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3913335 144781 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
134142839 144841 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913855 144841 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134143635 145029 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3915269 145029 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
134143366 145215 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3916659 145215 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134142204 145392 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3918046 145392 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11584702 145646 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3920049 145646 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134140270 145828 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3921499 145828 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134139279 145902 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922056 145902 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134139286 146009 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922810 146009 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134141886 146573 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3927481 146573 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
117812380 147207 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3932408 147207 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138595 147210 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
CHEMBL3932434 147210 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
134138824 147470 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934402 147470 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148504 147810 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3937200 147810 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149306 147930 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3938104 147930 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134145791 148242 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3940705 148242 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134145564 148546 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3943086 148546 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134147441 148945 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3946348 148945 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134155239 150470 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3958460 150470 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
134155132 150548 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959108 150548 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
134154079 151859 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970499 151859 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
134153247 152176 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3973085 152176 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
44570763 189655 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 449 4 1 4 2.7 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(F)ccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL517543 189655 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 449 4 1 4 2.7 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(F)ccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
9890504 89296 0 None - 1 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 461 10 3 10 -0.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)N1CC[C@@H](O)C1 10.1021/jm7010595
CHEMBL237699 89296 0 None - 1 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 461 10 3 10 -0.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)N1CC[C@@H](O)C1 10.1021/jm7010595
24969109 88433 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cccc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364338 88433 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cccc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
11518200 88448 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364353 88448 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11641108 88477 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364382 88477 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197887 88498 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364403 88498 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44447856 161253 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 558 15 4 12 1.6 Cc1noc(C)c1-c1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL414394 161253 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 558 15 4 12 1.6 Cc1noc(C)c1-c1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156018364 177329 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177329 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156022090 177619 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4649603 177619 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
10323604 10197 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161828 10197 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10323604 10197 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161828 10197 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44447853 94510 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 493 15 4 11 0.3 COc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254565 94510 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 493 15 4 11 0.3 COc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
25022503 155011 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 540 15 4 11 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1cccnc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL404355 155011 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 540 15 4 11 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1cccnc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44269035 27110 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13675 27110 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44269039 97876 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL275093 97876 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
145956061 162131 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162131 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
44570965 189235 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 418 4 2 6 0.8 Cc1ccc(-c2ccc(S(=O)(=O)N3CCNC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL516602 189235 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 418 4 2 6 0.8 Cc1ccc(-c2ccc(S(=O)(=O)N3CCNC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
69194933 88520 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 5 2 5 5.0 Cc1csc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3C)cc2)c1 10.6019/CHEMBL2364335
CHEMBL2364424 88520 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 5 2 5 5.0 Cc1csc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3C)cc2)c1 10.6019/CHEMBL2364335
69198297 88529 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364432 88529 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44447850 94481 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 488 14 4 11 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C#N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254363 94481 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 488 14 4 11 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C#N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44450015 95858 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 475 16 4 9 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL261358 95858 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 475 16 4 9 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCO 10.1016/j.bmcl.2008.03.059
178024 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
5867 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
CHEMBL13817 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
178024 1932 30 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
5867 1932 30 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
CHEMBL13817 1932 30 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
178024 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
5867 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
CHEMBL13817 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
145956061 162131 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162131 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
44450104 95344 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 496 14 4 10 -1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(N)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL258761 95344 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 496 14 4 10 -1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(N)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL500468 212334 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.03.059
CHEMBL500468 212334 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm300414b
22888475 63479 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 523 9 1 6 5.4 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C=O)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180246 63479 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 523 9 1 6 5.4 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C=O)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL500468 212334 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2005.02.040
162653916 179953 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753794 179953 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL500468 212334 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.02.021
CHEMBL500468 212334 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.05.100
178024 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
5867 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
CHEMBL13817 1932 30 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
156012849 176714 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 176714 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44390996 63958 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(C(F)(F)F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181063 63958 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(C(F)(F)F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11353414 64270 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181764 64270 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11353414 64270 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181764 64270 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44347919 16182 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 606 14 3 6 4.2 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122939 16182 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 606 14 3 6 4.2 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
16133832 211573 15 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
CHEMBL425281 211573 15 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
145957574 161739 0 None 57 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 161739 0 None 57 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
9875705 203580 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL79263 203580 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
156012849 176714 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 176714 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156013219 176905 0 None 60 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 176905 0 None 60 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11648350 88476 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364381 88476 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
59007043 88479 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(Cl)cccc2c1 10.6019/CHEMBL2364335
CHEMBL2364384 88479 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(Cl)cccc2c1 10.6019/CHEMBL2364335
69197106 88522 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)s3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364426 88522 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)s3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
24803348 88527 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364430 88527 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1F 10.6019/CHEMBL2364335
69197228 88573 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.6 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364475 88573 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.6 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
16114291 190690 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL5190973 190690 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/acs.jmedchem.1c02191
16114292 96473 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
CHEMBL266063 96473 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
9875705 203580 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL79263 203580 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
44436850 91104 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240509 91104 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44447840 94538 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254766 94538 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44447854 94511 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 469 14 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCC1CCCCC1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254566 94511 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 469 14 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCC1CCCCC1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL105462 206716 34 None 12 2 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm980197u
44447844 94423 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1cccc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL253965 94423 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1cccc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44450017 95886 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 15 4 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL261544 95886 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 15 4 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
10118326 23874 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL133848 23874 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
10458218 27265 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13687 27265 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
10745618 112475 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 568 13 2 4 4.5 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CC1 10.1021/jm980197u
CHEMBL331093 112475 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 568 13 2 4 4.5 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CC1 10.1021/jm980197u
10118326 23874 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL133848 23874 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
156010457 176470 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4632657 176470 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
23649669 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL398372 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
23649669 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1021/jm7010595
CHEMBL398372 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1021/jm7010595
23649669 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
CHEMBL398372 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
23649669 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL398372 153421 7 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44437955 10212 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162063 10212 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
10626337 100742 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL295984 100742 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
156010457 176470 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4632657 176470 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
156012445 176751 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 176751 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015928 176997 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 176997 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44452750 95797 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 7 2 6 4.4 COc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL261030 95797 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 7 2 6 4.4 COc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
44452932 97125 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1F 10.1016/j.bmcl.2007.12.021
CHEMBL270790 97125 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1F 10.1016/j.bmcl.2007.12.021
44570700 183367 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 486 6 2 6 2.1 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2)c1 10.1016/j.bmcl.2008.12.042
CHEMBL481620 183367 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 486 6 2 6 2.1 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2)c1 10.1016/j.bmcl.2008.12.042
69197169 88494 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364399 88494 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11641478 88502 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)s1 10.6019/CHEMBL2364335
CHEMBL2364407 88502 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)s1 10.6019/CHEMBL2364335
24803350 88538 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364441 88538 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1C 10.6019/CHEMBL2364335
11547664 88578 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364480 88578 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)c(F)c1 10.6019/CHEMBL2364335
44579802 186176 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488965 186176 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44444572 93572 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248745 93572 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
145962494 161513 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 161513 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145951150 162214 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162214 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
44434120 89463 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237926 89463 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
9827234 5249 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 498 9 5 4 3.1 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1c[nH]c2ccccc12)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL106841 5249 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 498 9 5 4 3.1 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1c[nH]c2ccccc12)C1CCNCC1 10.1016/j.bmc.2007.01.057
44411718 10194 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161825 10194 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44437953 10211 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162062 10211 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
44293557 100606 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL294923 100606 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL540001 100606 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
127046473 139237 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798645 139237 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
156012203 176750 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
CHEMBL4637255 176750 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
156016696 177046 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177046 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11525404 94924 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL256808 94924 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
44571004 183454 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 5 1 5 2.6 CNC1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccc(C)o3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL482203 183454 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 5 1 5 2.6 CNC1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccc(C)o3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL105462 206716 34 None 12 2 Rat 8.0 pEC50 = 8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/s0960-894x(97)10199-8
24969294 88438 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 460 5 3 6 3.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)c[nH]c3=O)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364343 88438 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 460 5 3 6 3.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)c[nH]c3=O)cc2F)o1 10.6019/CHEMBL2364335
69194607 88453 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1 10.6019/CHEMBL2364335
CHEMBL2364358 88453 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1 10.6019/CHEMBL2364335
69197049 88454 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364359 88454 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
69195141 88472 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 431 5 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1csc2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364377 88472 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 431 5 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1csc2ccccc12 10.6019/CHEMBL2364335
11682686 88485 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc4ccccc34)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364390 88485 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc4ccccc34)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69198021 88528 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccc(Cl)c12 10.6019/CHEMBL2364335
CHEMBL2364431 88528 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccc(Cl)c12 10.6019/CHEMBL2364335
11655608 88541 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364444 88541 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194649 88575 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364477 88575 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69196750 88577 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)nc1 10.6019/CHEMBL2364335
CHEMBL2364479 88577 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)nc1 10.6019/CHEMBL2364335
23730339 147575 0 None - 1 Human 8.0 pEC50 = 8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 10 3 10 0.4 CC1(O)CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
CHEMBL393531 147575 0 None - 1 Human 8.0 pEC50 = 8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 10 3 10 0.4 CC1(O)CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
156016696 177046 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177046 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145993528 166753 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294083 166753 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
156012203 176750 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
CHEMBL4637255 176750 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
145950201 162380 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 162380 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44281466 168805 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL442151 168805 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44452806 96222 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 486 7 2 7 4.6 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL263916 96222 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 486 7 2 7 4.6 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
44452885 97352 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 8 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL271948 97352 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 8 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
11633712 158776 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 446 5 2 6 3.9 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL410013 158776 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 446 5 2 6 3.9 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
57390496 68698 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 68698 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
56926782 68700 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923631 68700 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926785 68703 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923634 68703 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926892 68705 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923636 68705 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926893 68706 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
CHEMBL1923637 68706 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
134131183 141924 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890296 141924 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134133488 142692 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3896536 142692 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134870 143847 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3905987 143847 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134132958 144116 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
CHEMBL3908264 144116 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
134132265 144426 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
CHEMBL3910661 144426 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
76460236 144915 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3914338 144915 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134141159 146184 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3924192 146184 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149092 147909 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3937924 147909 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134146570 148236 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3940653 148236 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145820 148490 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3942642 148490 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155024 150468 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3958451 150468 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155282 150798 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961108 150798 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134152627 151004 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3963078 151004 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134150696 151535 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967506 151535 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134150029 151571 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967783 151571 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134153608 151826 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3970180 151826 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154022 152281 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3973940 152281 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134151899 152773 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3978207 152773 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
134156625 153105 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3981072 153105 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
16040587 178794 0 None -14 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm801332q
CHEMBL473921 178794 0 None -14 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm801332q
44576247 212441 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
CHEMBL506986 212441 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
44576247 212441 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL506986 212441 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL3578015 210009 0 None -33 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578018 210012 0 None -15 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
69198097 88459 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364364 88459 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)cc1 10.6019/CHEMBL2364335
69198438 88461 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)s1 10.6019/CHEMBL2364335
CHEMBL2364366 88461 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)s1 10.6019/CHEMBL2364335
69196473 88470 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 5 2 6 4.3 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)ccc2C#N)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364375 88470 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 5 2 6 4.3 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)ccc2C#N)C[C@@H](C)N1 10.6019/CHEMBL2364335
69197657 88471 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 497 8 2 7 4.5 COc1ccc(Oc2cccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364376 88471 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 497 8 2 7 4.5 COc1ccc(Oc2cccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)c2)cc1 10.6019/CHEMBL2364335
69195983 88492 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364397 88492 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196844 88509 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364414 88509 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11647817 88513 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 437 4 2 4 3.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.6019/CHEMBL2364335
CHEMBL2364418 88513 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 437 4 2 4 3.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.6019/CHEMBL2364335
69196864 88531 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(F)cc2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364434 88531 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(F)cc2F)cc1 10.6019/CHEMBL2364335
69198407 88560 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 5 2 5 3.6 COc1cc(Br)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364463 88560 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 5 2 5 3.6 COc1cc(Br)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
44579958 190738 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519171 190738 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
156020713 177504 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
CHEMBL4647751 177504 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
134139753 145491 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3918783 145491 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
44449923 95878 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 601 17 4 11 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(S(=O)(=O)CCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL261497 95878 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 601 17 4 11 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(S(=O)(=O)CCO)c1 10.1016/j.bmcl.2008.03.059
156020713 177504 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
CHEMBL4647751 177504 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
44434110 88070 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235135 88070 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL3578018 210012 0 None -15 2 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44450102 95314 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCO 10.1016/j.bmcl.2008.03.059
CHEMBL258550 95314 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCO 10.1016/j.bmcl.2008.03.059
16114290 136671 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374992 136671 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11664206 68696 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923626 68696 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
71453489 207613 13 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
9870965 63968 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 509 9 1 5 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181092 63968 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 509 9 1 5 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44434051 88971 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237058 88971 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
44434053 146313 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1cccc(NS(C)(=O)=O)c1 10.1016/j.bmcl.2007.07.099
CHEMBL392522 146313 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1cccc(NS(C)(=O)=O)c1 10.1016/j.bmcl.2007.07.099
145988557 166696 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4292914 166696 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL2170775 207608 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434083 89586 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL238155 89586 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
44436884 91107 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240522 91107 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
16114098 141067 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL385131 141067 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113246 94226 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252643 94226 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
22888486 63972 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 552 9 2 6 5.5 CC(=O)Nc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL181108 63972 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 552 9 2 6 5.5 CC(=O)Nc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
71453489 207613 13 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02122
CHEMBL2170781 207613 13 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02122
156018539 177225 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4643595 177225 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
145949755 162372 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162372 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
156013970 176656 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
CHEMBL4635743 176656 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
156018539 177225 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4643595 177225 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
69197178 88431 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(Cl)s2)cc1 10.6019/CHEMBL2364335
CHEMBL2364336 88431 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(Cl)s2)cc1 10.6019/CHEMBL2364335
69194396 88482 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 7 2 6 4.8 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364387 88482 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 7 2 6 4.8 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
69195258 88514 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 6 2 7 4.0 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364419 88514 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 6 2 7 4.0 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11604627 88530 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364433 88530 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197381 88548 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 486 6 2 7 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364451 88548 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 486 6 2 7 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
11576185 88555 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2nccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364458 88555 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2nccs2)cc1 10.6019/CHEMBL2364335
11633856 88581 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ncccn2)cc1 10.6019/CHEMBL2364335
CHEMBL2364483 88581 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ncccn2)cc1 10.6019/CHEMBL2364335
59007104 88584 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 1 6 4.8 COc1ccc(N2C[C@H](C)N(C)[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364486 88584 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 1 6 4.8 COc1ccc(N2C[C@H](C)N(C)[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2170779 207611 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44579824 183518 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482623 183518 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
44579883 186245 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489403 186245 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
44579861 192908 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL528332 192908 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
44579906 192009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL521612 192009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
145992125 166186 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4283504 166186 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
156016682 177182 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4642860 177182 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL2170776 207609 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(C(C)(C)C)cc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
16752689 187774 0 None -5 3 Rabbit 6.9 pEC50 = 6.9 Functional
Activity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assayActivity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assay
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1016/j.bmcl.2008.10.071
CHEMBL501315 187774 0 None -5 3 Rabbit 6.9 pEC50 = 6.9 Functional
Activity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assayActivity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assay
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1016/j.bmcl.2008.10.071
44444557 154136 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL399704 154136 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
145957404 161488 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
CHEMBL4160261 161488 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
145955250 161962 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167776 161962 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
145950261 162167 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162167 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156014569 176648 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4635694 176648 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
44452776 95868 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL261466 95868 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.021
69196695 88444 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 7 2 6 4.5 COc1ccc(NS(=O)(=O)c2ccc(Oc3ccccc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364349 88444 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 7 2 6 4.5 COc1ccc(NS(=O)(=O)c2ccc(Oc3ccccc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
59007058 88452 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)s1 10.6019/CHEMBL2364335
CHEMBL2364357 88452 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)s1 10.6019/CHEMBL2364335
156016682 177182 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4642860 177182 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44579842 184158 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL485091 184158 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
145986461 166649 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4291926 166649 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
145950261 162167 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162167 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
10602593 112331 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 542 12 2 4 4.1 CCNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL330860 112331 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 542 12 2 4 4.1 CCNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391038 64239 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 13 1 4 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181627 64239 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 13 1 4 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170783 207615 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](N)CCCCN)C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/jm300414b
CHEMBL2170779 207611 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156013970 176656 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
CHEMBL4635743 176656 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
156014569 176648 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4635694 176648 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
56926173 68655 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923501 68655 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
134138625 147486 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3934561 147486 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
155526063 170459 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4456830 170459 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145957404 161488 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
CHEMBL4160261 161488 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
145955250 161962 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167776 161962 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
44454060 154781 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 154781 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
57399248 68687 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923617 68687 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
145949755 162372 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162372 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
44434109 145736 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392076 145736 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
9890375 97805 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL274599 97805 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL558802 97805 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
44436876 146474 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL392663 146474 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
9890375 97805 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL274599 97805 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL558802 97805 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
9890375 97805 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL274599 97805 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL558802 97805 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
44281466 168805 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL442151 168805 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
162672839 182430 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4793824 182430 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
22888428 64004 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 508 9 2 4 4.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)NC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181247 64004 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 508 9 2 4 4.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)NC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
23730227 147329 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 15 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO 10.1021/jm7010595
CHEMBL393330 147329 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 15 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO 10.1021/jm7010595
44450133 159834 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 481 13 3 10 -0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL411122 159834 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 481 13 3 10 -0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
44579821 183636 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL483455 183636 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1Cl 10.1016/j.bmcl.2008.07.120
44579879 186402 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL490627 186402 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
44450071 96124 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 15 3 10 0.6 CCOC(=O)CCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL263141 96124 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 15 3 10 0.6 CCOC(=O)CCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
16113906 136686 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL375102 136686 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
44579752 186367 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 377 8 1 4 3.7 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490390 186367 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 377 8 1 4 3.7 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
44436887 90514 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239464 90514 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44434076 89333 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
CHEMBL237717 89333 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
145952740 161939 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 161939 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
23648250 78738 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113327 78738 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
16113577 84498 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL223725 84498 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
162657465 180449 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759418 180449 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
44444574 93573 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1CCNC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248746 93573 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1CCNC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
145952740 161939 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 161939 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
11532288 96459 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 7 2.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL265950 96459 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 7 2.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2007.12.021
11576186 154674 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccn3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.1016/j.bmcl.2007.12.021
CHEMBL402632 154674 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccn3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.1016/j.bmcl.2007.12.021
44570964 183289 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 407 4 1 5 1.7 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481014 183289 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 407 4 1 5 1.7 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
44570921 183363 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481601 183363 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
59007073 88432 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)nc1 10.6019/CHEMBL2364335
CHEMBL2364337 88432 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)nc1 10.6019/CHEMBL2364335
69197749 88441 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc3ccccc3c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364346 88441 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc3ccccc3c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11682796 88443 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 6 2 5 3.3 COc1ccc(NS(=O)(=O)/C=C/c2ccccc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364348 88443 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 6 2 5 3.3 COc1ccc(NS(=O)(=O)/C=C/c2ccccc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198460 88455 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.6019/CHEMBL2364335
CHEMBL2364360 88455 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.6019/CHEMBL2364335
69198360 88463 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364368 88463 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11683967 88475 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cccs2)c1 10.6019/CHEMBL2364335
CHEMBL2364380 88475 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cccs2)c1 10.6019/CHEMBL2364335
69195261 88483 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 7 2 6 5.2 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364388 88483 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 7 2 6 5.2 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11516766 88487 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364392 88487 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11525161 88544 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 5 2 5 4.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364447 88544 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 5 2 5 4.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194533 88574 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(F)c(-c2ccco2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364476 88574 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(F)c(-c2ccco2)cc1F 10.6019/CHEMBL2364335
69197165 88586 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 3 6 3.6 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364488 88586 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 3 6 3.6 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
44579777 186391 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490601 186391 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44454432 154707 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 154707 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
44434112 168283 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL438154 168283 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44579908 186281 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489610 186281 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145954311 161924 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 161924 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44434124 88216 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC#N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235817 88216 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC#N)n1 10.1016/j.bmcl.2007.07.099
162659161 180799 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763471 180799 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44444556 93953 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
CHEMBL250973 93953 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
145950963 162244 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162244 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145952396 162441 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162441 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
156011695 176771 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4637585 176771 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
44452887 159019 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL410282 159019 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2007.12.021
46882522 5621 0 None -39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078208 5621 0 None -39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
69195349 88466 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Br)c1 10.6019/CHEMBL2364335
CHEMBL2364371 88466 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Br)c1 10.6019/CHEMBL2364335
69198352 88587 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364489 88587 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
44446188 154840 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403542 154840 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
145954311 161924 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 161924 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
46882521 5620 0 None -158 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078207 5620 0 None -158 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
44445620 154128 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399651 154128 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
22862453 97994 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
CHEMBL275795 97994 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
10675061 96083 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
CHEMBL262889 96083 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
10026738 162207 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL417182 162207 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL557206 162207 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
56926464 68682 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
CHEMBL1923612 68682 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
155540883 172378 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172378 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
10210658 10213 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL1162064 10213 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
145952396 162441 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162441 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL2170784 207616 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
134139080 147138 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3931856 147138 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
156011695 176771 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4637585 176771 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL2170697 207602 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434080 89467 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44434080 89467 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL237933 89467 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237933 89467 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
10210658 10213 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL1162064 10213 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
10026738 162207 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL417182 162207 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL557206 162207 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
10530983 167810 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 564 11 2 4 4.0 CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL434609 167810 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 564 11 2 4 4.0 CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391003 122792 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 531 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL361612 122792 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 531 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170780 207612 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
145950963 162244 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162244 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
127047409 139088 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797639 139088 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
10745533 139577 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL380096 139577 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
44437971 200824 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611489 200824 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
16113693 137476 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376471 137476 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
11692516 68691 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923621 68691 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
155557019 174005 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174005 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
9810101 98779 12 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL281764 98779 12 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10745533 139577 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL380096 139577 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
44437971 200824 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611489 200824 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44579909 186310 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489819 186310 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44436882 145471 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL391859 145471 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL2170698 207603 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434122 89067 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCCC#N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237302 89067 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCCC#N)n1 10.1016/j.bmcl.2007.07.099
145992142 166207 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4283858 166207 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL3578006 210003 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm501702q
145953016 162025 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162025 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
44454304 97141 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL270876 97141 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454092 97187 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97187 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454338 97373 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL272085 97373 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
22867310 29812 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 4 4 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2O 10.1016/s0960-894x(97)10199-8
CHEMBL13891 29812 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 4 4 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2O 10.1016/s0960-894x(97)10199-8
162653802 179939 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753592 179939 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44436886 161394 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL415674 161394 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
9987037 11912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183385 11912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL294324 11912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
44391008 64521 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 9 1 5 4.6 CCN(CC)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182137 64521 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 9 1 5 4.6 CCN(CC)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
22888379 167739 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 584 12 2 5 4.8 CC(=O)NC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL434152 167739 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 584 12 2 5 4.8 CC(=O)NC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
44444564 94023 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1cccc(-c3ccccn3)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251366 94023 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1cccc(-c3ccccn3)c1)CC2 10.1016/j.bmcl.2007.09.067
145961213 161602 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162174 161602 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
145953016 162025 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162025 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145949595 162162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145974293 162462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 162462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44452929 97081 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccco2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL270573 97081 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccco2)c1 10.1016/j.bmcl.2007.12.021
46882396 5752 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc(C)[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079187 5752 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc(C)[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
44570698 183366 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 456 5 2 5 2.0 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481619 183366 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 456 5 2 5 2.0 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
24969292 88435 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccn3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364340 88435 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccn3)cc2F)o1 10.6019/CHEMBL2364335
69194665 88468 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 3.9 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.6019/CHEMBL2364335
CHEMBL2364373 88468 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 3.9 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.6019/CHEMBL2364335
11524465 88488 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 413 4 2 4 4.0 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364393 88488 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 413 4 2 4 4.0 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11576404 88499 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364404 88499 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69194865 88518 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364422 88518 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2ccccc12 10.6019/CHEMBL2364335
11712498 88532 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364435 88532 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2F)cc1 10.6019/CHEMBL2364335
69195296 88537 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3F)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364440 88537 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3F)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11518242 88540 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.9 Cc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364443 88540 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.9 Cc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
69197366 88545 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364448 88545 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11503413 88562 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 454 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccn2C)cc1 10.6019/CHEMBL2364335
CHEMBL2364465 88562 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 454 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccn2C)cc1 10.6019/CHEMBL2364335
11647900 88568 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1cc(-c2ccco2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364470 88568 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1cc(-c2ccco2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
11669734 88569 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364471 88569 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
44391007 64520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 480 9 1 4 4.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182136 64520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 480 9 1 4 4.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
145994050 166780 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4294493 166780 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
156016392 177062 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177062 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL3578006 210003 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm501702q
25098836 190852 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519322 190852 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145957574 161739 0 None 57 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 161739 0 None 57 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
44411745 10196 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161827 10196 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
10626337 100742 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL295984 100742 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
156013219 176905 0 None 60 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 176905 0 None 60 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
22888352 63591 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180659 63591 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888352 63591 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180659 63591 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
10649999 16910 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL125498 16910 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
156015928 176997 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 176997 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156012445 176751 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 176751 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44411634 10193 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161824 10193 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44411634 10193 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161824 10193 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44390986 64323 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccccc1CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181832 64323 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccccc1CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170695 207600 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156011766 176724 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4636780 176724 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
44281449 112882 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33182 112882 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
44281449 112882 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33182 112882 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
23648249 78737 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113326 78737 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
10166594 64290 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181786 64290 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391010 64528 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 9 1 6 6.3 CSc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL182158 64528 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 9 1 6 6.3 CSc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
23648244 91568 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241775 91568 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
155557019 174005 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174005 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44444565 94051 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 474 5 1 8 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccon3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251573 94051 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 474 5 1 8 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccon3)s1)CC2 10.1016/j.bmcl.2007.09.067
145957075 161717 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 161717 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44411745 10196 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161827 10196 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
156013684 176681 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636178 176681 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156011766 176724 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4636780 176724 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
11539642 97466 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 448 6 2 8 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL272540 97466 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 448 6 2 8 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)s1 10.1016/j.bmcl.2007.12.021
44570702 183244 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 463 4 1 5 3.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480639 183244 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 463 4 1 5 3.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
11683968 88474 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364379 88474 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197883 88497 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2F)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364402 88497 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2F)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69195597 88510 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2Cl)s1 10.6019/CHEMBL2364335
CHEMBL2364415 88510 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2Cl)s1 10.6019/CHEMBL2364335
59007081 88524 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 5 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(Cl)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364428 88524 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 5 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(Cl)c2)cc1 10.6019/CHEMBL2364335
11648834 88579 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364481 88579 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1F 10.6019/CHEMBL2364335
44411753 10198 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161829 10198 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
44411753 10198 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161829 10198 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
10415000 167493 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL432461 167493 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
71453489 207613 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156013684 176681 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636178 176681 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
10415000 167493 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL432461 167493 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
156019457 177358 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177358 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44449922 95761 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 615 17 3 11 1.0 CN(CCc1cccc(S(=O)(=O)CCO)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL260849 95761 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 615 17 3 11 1.0 CN(CCc1cccc(S(=O)(=O)CCO)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
44269019 97761 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL274340 97761 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44579840 184156 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL485090 184156 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579907 186455 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491044 186455 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
44579805 186473 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL491221 186473 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44434113 88207 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235793 88207 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
127048060 139318 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799222 139318 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
57399248 68687 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923617 68687 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44268965 23843 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2=O)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13383 23843 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2=O)C1 10.1016/s0960-894x(97)10199-8
10675800 113282 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 654 11 2 4 4.3 CNC(=O)[C@@H](Cc1ccc(I)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL332414 113282 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 654 11 2 4 4.3 CNC(=O)[C@@H](Cc1ccc(I)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391002 123379 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 507 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL362798 123379 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 507 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44579857 186331 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL490009 186331 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
44434018 88050 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 399 8 3 8 0.9 COC(=O)CCn1nnnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235012 88050 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 399 8 3 8 0.9 COC(=O)CCn1nnnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44579641 186304 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 370 7 1 4 4.0 CSc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489794 186304 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 370 7 1 4 4.0 CSc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
44579996 186543 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 367 7 2 4 2.8 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)COc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491835 186543 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 367 7 2 4 2.8 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)COc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
44579919 190745 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 444 9 1 4 5.3 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(-c2ccccc2)c1OC 10.1016/j.bmcl.2008.07.120
CHEMBL519196 190745 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 444 9 1 4 5.3 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(-c2ccccc2)c1OC 10.1016/j.bmcl.2008.07.120
44454092 97187 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97187 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44450070 158093 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 14 4 9 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(=O)O 10.1016/j.bmcl.2008.03.059
CHEMBL409258 158093 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 14 4 9 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(=O)O 10.1016/j.bmcl.2008.03.059
156016392 177062 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177062 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145961213 161602 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162174 161602 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
145949595 162162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145974293 162462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 162462 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44390905 64111 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 544 10 1 6 3.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181337 64111 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 544 10 1 6 3.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391040 64115 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 577 10 1 6 5.0 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181352 64115 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 577 10 1 6 5.0 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10579444 113731 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
CHEMBL332987 113731 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
162645413 179136 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744051 179136 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
44293091 187593 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL49884 187593 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
16114011 137597 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL376736 137597 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
145981343 166145 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4282719 166145 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44391048 62604 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 8 2 5 4.2 CC(C)NCCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178502 62604 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 8 2 5 4.2 CC(C)NCCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
44454399 154588 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL402086 154588 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
44293091 187593 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL49884 187593 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
155540883 172378 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172378 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44579801 186568 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL492028 186568 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
168276220 189817 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 261 6 1 1 4.2 CCCCCCCc1cc(=O)c2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5177954 189817 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 261 6 1 1 4.2 CCCCCCCc1cc(=O)c2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
145958774 161704 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 161704 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145950877 162433 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162433 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44450135 158145 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL409327 158145 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2008.03.059
44454302 158821 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL410060 158821 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
16203237 96490 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
CHEMBL266199 96490 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
56926462 68680 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923610 68680 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
162660604 180627 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761319 180627 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
145956753 161596 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162000 161596 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
71453489 207613 13 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44446190 94107 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL251855 94107 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44446189 154823 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403426 154823 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
10744738 16013 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1cccc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122420 16013 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1cccc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL2170699 207604 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44454432 154707 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 154707 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
44454397 154972 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC(C#N)Cc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL404227 154972 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC(C#N)Cc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
145949381 162153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
22862431 30255 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL13930 30255 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1016/s0960-894x(97)10199-8
162653781 179890 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753046 179890 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
156013764 176687 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636229 176687 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
145958317 161751 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 161751 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145949381 162153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950877 162433 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162433 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
156013764 176687 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636229 176687 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156020452 177450 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646979 177450 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
24969201 88439 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364344 88439 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1Cl 10.6019/CHEMBL2364335
69197403 88464 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 5 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc2cc(Cl)ccc2s1 10.6019/CHEMBL2364335
CHEMBL2364369 88464 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 5 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc2cc(Cl)ccc2s1 10.6019/CHEMBL2364335
59007071 88478 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 3 7 3.5 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364383 88478 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 3 7 3.5 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11547135 88491 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 2 5 5.1 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)s4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364396 88491 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 2 5 5.1 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)s4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11567764 88495 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 411 5 2 6 2.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-n4cccn4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364400 88495 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 411 5 2 6 2.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-n4cccn4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11511157 88505 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2C)s1 10.6019/CHEMBL2364335
CHEMBL2364410 88505 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2C)s1 10.6019/CHEMBL2364335
11547599 88507 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(NS(=O)(=O)c2ccc(-c3c(C)cccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364412 88507 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(NS(=O)(=O)c2ccc(-c3c(C)cccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197133 88517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)s1 10.6019/CHEMBL2364335
CHEMBL2364421 88517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)s1 10.6019/CHEMBL2364335
69197849 88542 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 429 5 2 5 4.1 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364445 88542 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 429 5 2 5 4.1 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69198350 88549 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 9 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csnn2)s1 10.6019/CHEMBL2364335
CHEMBL2364452 88549 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 9 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csnn2)s1 10.6019/CHEMBL2364335
156020452 177450 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646979 177450 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44579860 188304 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL507551 188304 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145956415 161502 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 161502 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145956415 161502 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 161502 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145956753 161596 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162000 161596 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145958774 161704 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 161704 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145955718 161973 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4167965 161973 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145952404 162174 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171300 162174 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL3578014 210008 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44436816 91359 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241242 91359 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44391028 63952 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 451 9 1 4 3.9 CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181051 63952 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 451 9 1 4 3.9 CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44390906 131568 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 7 2 5 4.2 CC(C)(CN)CNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL369571 131568 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 7 2 5 4.2 CC(C)(CN)CNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
44434052 88972 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccc(NS(C)(=O)=O)cc1 10.1016/j.bmcl.2007.07.099
CHEMBL237059 88972 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccc(NS(C)(=O)=O)cc1 10.1016/j.bmcl.2007.07.099
44450169 159191 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 471 12 3 8 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCC(F)(F)F 10.1016/j.bmcl.2008.03.059
CHEMBL410499 159191 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 471 12 3 8 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCC(F)(F)F 10.1016/j.bmcl.2008.03.059
56926894 68707 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923638 68707 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
44391027 128268 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 12 1 4 5.6 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL366916 128268 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 12 1 4 5.6 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44579803 186177 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488966 186177 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145952404 162174 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171300 162174 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL3578014 210008 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
11526696 71243 13 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
CHEMBL1923502 71243 13 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
CHEMBL1963249 71243 13 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
44450045 158678 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL409894 158678 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCO 10.1016/j.bmcl.2008.03.059
44434012 88631 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL236513 88631 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44454398 97136 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL270851 97136 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
11526745 68711 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923642 68711 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
44391020 63518 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180337 63518 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
162643920 181188 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4777792 181188 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
155540883 172378 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172378 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145955718 161973 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4167965 161973 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
23648236 78727 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
CHEMBL2113317 78727 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
145958317 161751 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 161751 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
162649014 179351 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4746362 179351 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
44434123 145005 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
CHEMBL391510 145005 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
11526696 71243 13 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923502 71243 13 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1963249 71243 13 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
122178179 120737 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578008 120737 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
145980382 166079 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4281310 166079 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71453489 207613 13 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
134149793 148061 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
CHEMBL3939196 148061 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
145980333 166017 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4280040 166017 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44579823 183489 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482420 183489 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145957075 161717 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 161717 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145951150 162214 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162214 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
44449864 158272 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCCCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL409462 158272 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCCCO)c1 10.1016/j.bmcl.2008.03.059
10005618 10210 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162058 10210 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
15481181 77376 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL209020 77376 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
9810101 98779 12 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL281764 98779 12 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
15481188 140666 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL382844 140666 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL130229 206935 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmc.2007.01.057
16114292 96473 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL266063 96473 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
16114292 96473 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 96473 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
23730225 153630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 435 12 4 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCO 10.1021/jm7010595
CHEMBL398570 153630 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 435 12 4 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCO 10.1021/jm7010595
10530781 15387 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 554 12 2 4 4.2 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122108 15387 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 554 12 2 4 4.2 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10005618 10210 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162058 10210 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
15481181 77376 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL209020 77376 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
9810101 98779 12 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL281764 98779 12 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
15481188 140666 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL382844 140666 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL130229 206935 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmc.2007.01.057
156011385 176794 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637916 176794 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44449956 96154 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 523 14 3 9 2.0 CN(CCc1cccc(O)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL263389 96154 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 523 14 3 9 2.0 CN(CCc1cccc(O)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
44447846 94445 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1cccc(OC(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254166 94445 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1cccc(OC(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44444566 154217 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL400124 154217 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156011385 176794 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637916 176794 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156019457 177358 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177358 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44570961 191952 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.2 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)c(F)c2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL521246 191952 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.2 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)c(F)c2)C1 10.1016/j.bmcl.2008.12.042
69195095 88521 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)c(F)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364425 88521 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)c(F)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69194503 88557 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364460 88557 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1Cl 10.6019/CHEMBL2364335
59007103 88583 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cn1 10.6019/CHEMBL2364335
CHEMBL2364485 88583 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cn1 10.6019/CHEMBL2364335
69197358 88589 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 3 6 4.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364491 88589 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 3 6 4.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2F)o1 10.6019/CHEMBL2364335
44450046 95399 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 501 14 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCN1CCNC1=O 10.1016/j.bmcl.2008.03.059
CHEMBL259016 95399 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 501 14 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCN1CCNC1=O 10.1016/j.bmcl.2008.03.059
23730341 89298 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 502 11 3 10 0.1 CC(=O)N[C@@H]1CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
CHEMBL237701 89298 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 502 11 3 10 0.1 CC(=O)N[C@@H]1CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
71453489 207613 13 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44390914 63292 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 11 1 5 4.9 CCCOC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180093 63292 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 11 1 5 4.9 CCCOC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888424 122469 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 11 1 4 5.7 CC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL360877 122469 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 11 1 4 5.7 CC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
71453489 207613 13 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
162671996 182239 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4791255 182239 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
23730228 89148 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 14 3 10 0.6 CN(CCCCO)C(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
CHEMBL237492 89148 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 14 3 10 0.6 CN(CCCCO)C(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
71453489 207613 13 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44444568 93531 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248542 93531 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
15481185 76893 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL207970 76893 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
156011736 176839 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4638566 176839 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
25022506 94810 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL256263 94810 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2007.12.021
24803347 154477 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL401548 154477 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1 10.1016/j.bmcl.2007.12.021
46882394 5750 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079185 5750 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
46882395 5751 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2[nH]cnc2C)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079186 5751 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2[nH]cnc2C)CC3)cc1 10.1016/j.bmcl.2009.09.027
44570699 190701 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 474 5 2 5 2.2 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL519121 190701 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 474 5 2 5 2.2 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
69196498 88469 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)s1 10.6019/CHEMBL2364335
CHEMBL2364374 88469 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)s1 10.6019/CHEMBL2364335
69197028 88508 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)c3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364413 88508 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)c3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198238 88519 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 2 5 4.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364423 88519 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 2 5 4.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11712867 88556 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364459 88556 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)cc1F 10.6019/CHEMBL2364335
69194471 88571 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364473 88571 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(F)c1 10.6019/CHEMBL2364335
11698505 88580 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364482 88580 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1 10.6019/CHEMBL2364335
9950632 88264 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
CHEMBL236038 88264 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
44579880 186243 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489401 186243 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
44579841 191945 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL521176 191945 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44434010 88331 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL236311 88331 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
9950632 88264 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
9950632 88264 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
CHEMBL236038 88264 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL236038 88264 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
44434010 88331 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL236311 88331 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44437966 200399 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL608827 200399 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437969 200823 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611488 200823 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437966 200399 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL608827 200399 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437969 200823 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611488 200823 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44454368 94805 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCC(C#N)c2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL256236 94805 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCC(C#N)c2ccccc2)n1 10.1016/j.bmcl.2008.01.100
145987684 166713 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4293331 166713 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44444560 154403 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 541 5 1 5 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)Cc1cccc(I)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL401133 154403 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 541 5 1 5 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)Cc1cccc(I)c1)CC2 10.1016/j.bmcl.2007.09.067
145953855 161953 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 161953 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44570923 183364 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 403 4 1 5 2.0 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481602 183364 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 403 4 1 5 2.0 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)cc2)C1 10.1016/j.bmcl.2008.12.042
44570761 189369 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 NC1CCN(C(=O)C2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL517081 189369 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 NC1CCN(C(=O)C2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
122178179 120737 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578008 120737 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
24969112 88434 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 7 3.2 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccnc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364339 88434 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 7 3.2 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccnc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
11540248 88440 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 6 4.9 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364345 88440 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 6 4.9 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11647560 88442 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2cccc3ccccc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364347 88442 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2cccc3ccccc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196005 88473 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1sc2ccc(F)cc2c1C 10.6019/CHEMBL2364335
CHEMBL2364378 88473 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1sc2ccc(F)cc2c1C 10.6019/CHEMBL2364335
69198434 88481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 488 7 2 8 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccc2OC)s1 10.6019/CHEMBL2364335
CHEMBL2364386 88481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 488 7 2 8 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccc2OC)s1 10.6019/CHEMBL2364335
69198286 88489 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 4 2 5 3.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cc4ccccc4s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364394 88489 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 4 2 5 3.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cc4ccccc4s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11562181 88500 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(F)c3F)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364405 88500 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(F)c3F)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196132 88511 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2)s1 10.6019/CHEMBL2364335
CHEMBL2364416 88511 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2)s1 10.6019/CHEMBL2364335
69197703 88512 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)cc2)s1 10.6019/CHEMBL2364335
CHEMBL2364417 88512 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)cc2)s1 10.6019/CHEMBL2364335
69194443 88533 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364436 88533 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2F)cc1 10.6019/CHEMBL2364335
11503069 88536 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 439 5 2 4 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364439 88536 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 439 5 2 4 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11647941 88543 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.4 Cc1cc(-c2ccoc2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364446 88543 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.4 Cc1cc(-c2ccoc2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
11576203 88550 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)CCC(C)(C)O2 10.6019/CHEMBL2364335
CHEMBL2364453 88550 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)CCC(C)(C)O2 10.6019/CHEMBL2364335
11683891 88564 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccn2)cc1 10.6019/CHEMBL2364335
CHEMBL2364467 88564 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccn2)cc1 10.6019/CHEMBL2364335
69194380 88588 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364490 88588 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
56926783 68701 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923632 68701 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
156021183 177540 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648308 177540 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156017268 177066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021183 177540 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648308 177540 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44453070 94637 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cncnc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL255401 94637 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cncnc2)cc1 10.1016/j.bmcl.2007.12.021
44453097 154542 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL401891 154542 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2007.12.021
44570762 182836 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 414 4 1 5 1.9 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cccnc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL479865 182836 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 414 4 1 5 1.9 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cccnc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL3578013 210007 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
156017268 177066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44434114 88974 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnc([C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237060 88974 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnc([C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)n1 10.1016/j.bmcl.2007.07.099
44450134 161331 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 479 13 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL415095 161331 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 479 13 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCc1ccccc1 10.1016/j.bmcl.2008.03.059
44446177 94197 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252448 94197 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL500468 212334 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/s0960-894x(01)00324-9
44450105 95345 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 507 15 3 8 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL258762 95345 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 507 15 3 8 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2008.03.059
44447848 94446 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(OC(F)(F)F)cc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254167 94446 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(OC(F)(F)F)cc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44580031 192458 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL522446 192458 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL3578013 210007 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44447845 94424 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 599 14 4 10 2.3 CC(C)(N)C(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL253966 94424 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 599 14 4 10 2.3 CC(C)(N)C(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44434119 89462 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
CHEMBL237925 89462 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
145953855 161953 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 161953 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44434121 89464 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL237927 89464 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
162646324 179146 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744139 179146 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
10721075 15363 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1csc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL121960 15363 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1csc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
145959787 161723 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16114289 98199 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL277376 98199 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
56926892 68705 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923636 68705 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
145984632 165827 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4276775 165827 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
155551597 173367 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4541252 173367 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
22862448 96717 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
CHEMBL268231 96717 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
22867465 96757 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/s0960-894x(97)10199-8
CHEMBL268518 96757 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/s0960-894x(97)10199-8
44301387 11144 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179088 11144 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL59572 11144 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
56926356 68662 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923512 68662 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
10143731 63982 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181156 63982 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44444558 167203 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 465 4 0 5 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL430398 167203 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 465 4 0 5 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
145959007 161695 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 161695 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145959787 161723 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156021766 177543 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 177543 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44452826 94925 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 428 5 2 6 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL256809 94925 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 428 5 2 6 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
44452777 95760 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 470 6 2 7 4.0 CC(=O)c1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL260831 95760 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 470 6 2 7 4.0 CC(=O)c1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
11554351 96079 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 6 2.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(N2CCCC2=O)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL262879 96079 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 6 2.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(N2CCCC2=O)cc1 10.1016/j.bmcl.2007.12.021
11605061 96253 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 462 5 2 6 4.5 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL264170 96253 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 462 5 2 6 4.5 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
44452825 154699 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 472 7 2 7 4.2 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL402772 154699 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 472 7 2 7 4.2 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL3578017 210011 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
69197033 88465 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364370 88465 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197513 88480 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 448 6 2 8 3.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364385 88480 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 448 6 2 8 3.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196509 88484 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364389 88484 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11669948 88496 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)c(C)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364401 88496 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)c(C)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196071 88554 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 478 6 2 8 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364457 88554 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 478 6 2 8 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)n2)s1 10.6019/CHEMBL2364335
69194899 88558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccoc2)c1 10.6019/CHEMBL2364335
CHEMBL2364461 88558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccoc2)c1 10.6019/CHEMBL2364335
44434055 88861 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL236858 88861 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
44436889 152511 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397594 152511 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44570922 191954 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 415 3 1 4 1.6 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL521264 191954 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 415 3 1 4 1.6 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.12.042
69196838 88445 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364350 88445 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
25211977 186309 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489818 186309 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
16113580 137340 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
CHEMBL376258 137340 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
44434111 145738 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392077 145738 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
15481185 76893 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL207970 76893 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
127048059 139023 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797225 139023 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
16113580 137340 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376258 137340 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44450103 95315 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 14 3 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL258551 95315 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 14 3 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
44391032 64499 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 8 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182050 64499 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 8 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
156011736 176839 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4638566 176839 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
44450132 95553 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL259712 95553 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCCCO 10.1016/j.bmcl.2008.03.059
145948725 166925 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299615 166925 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
44281450 99171 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL284295 99171 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44281450 99171 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL284295 99171 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44411584 10191 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161822 10191 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
156015766 176984 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4640438 176984 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
44411584 10191 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161822 10191 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
22888433 64267 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 535 10 1 5 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC1CCCCC1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181735 64267 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 535 10 1 5 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC1CCCCC1)C(C)C 10.1016/j.bmcl.2005.02.040
44579775 186587 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL492230 186587 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1 10.1016/j.bmcl.2008.07.120
11258291 188505 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL510195 188505 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579882 192454 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL522426 192454 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44450044 160543 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 433 13 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411699 160543 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 433 13 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCO 10.1016/j.bmcl.2008.03.059
56926463 68681 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923611 68681 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
145981687 166013 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4279987 166013 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44579640 186303 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 354 7 1 4 3.2 COc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489793 186303 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 354 7 1 4 3.2 COc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
44579686 186398 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 395 8 2 4 3.6 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(NC(C)=O)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490614 186398 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 395 8 2 4 3.6 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(NC(C)=O)cc1 10.1016/j.bmcl.2008.07.120
16203238 136572 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
CHEMBL374757 136572 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
44390997 122472 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 8 1 5 4.6 CC(C)N(C)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL360891 122472 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 8 1 5 4.6 CC(C)N(C)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL3578017 210011 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
23661656 168467 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 168467 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434074 154123 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL399625 154123 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434009 166882 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL429799 166882 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
22867312 23651 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2=O 10.1016/s0960-894x(97)10199-8
CHEMBL13366 23651 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2=O 10.1016/s0960-894x(97)10199-8
162665952 181787 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4785149 181787 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44434056 144450 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL391088 144450 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434007 88133 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235446 88133 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
156021766 177543 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 177543 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44391035 122080 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 545 11 1 4 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL360247 122080 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 545 11 1 4 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
44301512 11902 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183340 11902 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL291333 11902 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
145979268 166100 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4281647 166100 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
145959007 161695 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 161695 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
44580030 186377 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 324 6 1 3 3.2 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL490422 186377 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 324 6 1 3 3.2 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
118718706 114867 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3350011 114867 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
44301462 11142 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179075 11142 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL58758 11142 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
16113800 137274 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL375972 137274 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44391015 123025 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL361802 123025 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
162677268 182981 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4800459 182981 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
10507433 16275 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 578 13 3 6 3.5 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL123430 16275 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 578 13 3 6 3.5 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
23730458 146027 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 499 14 3 11 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCn1ccnc1 10.1021/jm7010595
CHEMBL392296 146027 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 499 14 3 11 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCn1ccnc1 10.1021/jm7010595
44576247 212441 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL506986 212441 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
168285897 191051 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 273 7 1 2 4.1 CCCCCCCc1cc(=O)c2cc(OC)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5196194 191051 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 273 7 1 2 4.1 CCCCCCCc1cc(=O)c2cc(OC)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
155529391 170864 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4463042 170864 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145956659 161494 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 161494 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
155537651 171740 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4475293 171740 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145981196 165972 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4279344 165972 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
145979819 165909 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4278185 165909 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44434016 89748 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL238228 89748 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
16113692 136699 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL375162 136699 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
24970113 68699 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923629 68699 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL2170777 207610 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CCC[C@H](NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm300414b
145956026 162100 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162100 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
22862436 10202 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161834 10202 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10602640 137648 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
CHEMBL376970 137648 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
10791616 138993 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL379564 138993 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10029990 168707 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL441360 168707 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
11526696 71243 13 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923502 71243 13 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1963249 71243 13 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
10649323 15340 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 508 13 2 5 2.5 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](COCc1ccccc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL121803 15340 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 508 13 2 5 2.5 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](COCc1ccccc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10841400 16657 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 608 13 3 5 3.7 C[C@H](O)CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL124831 16657 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 608 13 3 5 3.7 C[C@H](O)CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
156009875 176539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 176539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44444562 94022 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 463 6 1 5 3.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)CCc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251365 94022 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 463 6 1 5 3.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)CCc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.09.067
145956026 162100 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162100 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
22862436 10202 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161834 10202 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10602640 137648 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
CHEMBL376970 137648 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
10791616 138993 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL379564 138993 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10029990 168707 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL441360 168707 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
156009875 176539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 176539 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015766 176984 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4640438 176984 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
44570967 189566 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL517391 189566 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
24969114 88437 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 506 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364342 88437 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 506 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1Cl 10.6019/CHEMBL2364335
59007076 88460 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364365 88460 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1 10.6019/CHEMBL2364335
69197196 88462 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)s1 10.6019/CHEMBL2364335
CHEMBL2364367 88462 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)s1 10.6019/CHEMBL2364335
69197071 88501 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364406 88501 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194482 88516 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
CHEMBL2364420 88516 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
11719784 88553 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364456 88553 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1C 10.6019/CHEMBL2364335
59007054 88585 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 3 6 3.9 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2)o1 10.6019/CHEMBL2364335
CHEMBL2364487 88585 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 3 6 3.9 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2)o1 10.6019/CHEMBL2364335
16114097 78732 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113321 78732 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
16113710 78736 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113325 78736 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
23730226 147327 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 449 13 4 10 -0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCO 10.1021/jm7010595
CHEMBL393329 147327 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 449 13 4 10 -0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCO 10.1021/jm7010595
71453489 207613 13 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
CHEMBL2170781 207613 13 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
44411632 10192 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161823 10192 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
22888425 62180 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(CO)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178216 62180 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(CO)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44411632 10192 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161823 10192 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL2170782 207614 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44579858 186332 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490010 186332 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)cc1 10.1016/j.bmcl.2008.07.120
44579778 186426 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490801 186426 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
162657606 180525 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760409 180525 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
145956659 161494 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 161494 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950987 162278 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4172848 162278 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
69198313 88456 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccnc12 10.6019/CHEMBL2364335
CHEMBL2364361 88456 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccnc12 10.6019/CHEMBL2364335
69195692 88457 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.6019/CHEMBL2364335
CHEMBL2364362 88457 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.6019/CHEMBL2364335
69196612 88458 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.6019/CHEMBL2364335
CHEMBL2364363 88458 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.6019/CHEMBL2364335
11511158 88506 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364411 88506 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198054 88559 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cc(C)cs2)c1 10.6019/CHEMBL2364335
CHEMBL2364462 88559 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cc(C)cs2)c1 10.6019/CHEMBL2364335
69195074 88572 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)nc1 10.6019/CHEMBL2364335
CHEMBL2364474 88572 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)nc1 10.6019/CHEMBL2364335
69195546 88582 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364484 88582 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c2ccccc12 10.6019/CHEMBL2364335
44580028 192637 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 416 8 1 4 4.5 COc1c(-c2ccccc2)cccc1N(C[C@H]1CCCN1)C(=O)COc1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL523786 192637 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 416 8 1 4 4.5 COc1c(-c2ccccc2)cccc1N(C[C@H]1CCCN1)C(=O)COc1ccccc1 10.1016/j.bmcl.2008.07.120
44434011 147319 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL393321 147319 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
57390496 68698 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 68698 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
145988894 166580 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4290680 166580 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44434086 148311 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C/C=C/c2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL394130 148311 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C/C=C/c2ccccc2)n1 10.1016/j.bmcl.2007.07.099
145950987 162278 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4172848 162278 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
44449924 159386 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 487 12 4 9 1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)N[C@H]1CC[C@H](O)CC1 10.1016/j.bmcl.2008.03.059
CHEMBL410730 159386 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 487 12 4 9 1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)N[C@H]1CC[C@H](O)CC1 10.1016/j.bmcl.2008.03.059
56926785 68703 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923634 68703 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434078 89466 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC2Cc3ccccc3N2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237932 89466 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC2Cc3ccccc3N2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434008 145989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL392268 145989 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44411913 10201 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161833 10201 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44268939 30218 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13926 30218 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44411913 10201 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161833 10201 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44434015 88049 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL235011 88049 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44411905 10200 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161832 10200 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10506325 100758 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL296104 100758 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
16113371 78728 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL2113318 78728 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
162676229 182712 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797064 182712 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL3578005 210002 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm501702q
44348031 112577 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 618 14 3 5 4.3 C[C@@H](O)CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL331303 112577 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 618 14 3 5 4.3 C[C@@H](O)CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44411905 10200 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161832 10200 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44437953 10211 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162062 10211 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
10506325 100758 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL296104 100758 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
44436857 145111 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL391588 145111 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
156021787 177559 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648799 177559 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
10006735 116499 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33892 116499 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
10006735 116499 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33892 116499 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
156021787 177559 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648799 177559 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
11712108 160749 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL412303 160749 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
44571003 191979 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 445 4 1 5 3.0 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL521439 191979 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 445 4 1 5 3.0 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL3578005 210002 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm501702q
69196876 88447 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 7 2.9 COc1ccc(NS(=O)(=O)c2ccc(-n3cccn3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364352 88447 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 7 2.9 COc1ccc(NS(=O)(=O)c2ccc(-n3cccn3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11562329 88486 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 495 8 2 6 4.5 COCc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.6019/CHEMBL2364335
CHEMBL2364391 88486 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 495 8 2 6 4.5 COCc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.6019/CHEMBL2364335
69196868 88490 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 2 5 4.4 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364395 88490 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 2 5 4.4 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69196990 88546 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 480 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364449 88546 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 480 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1C 10.6019/CHEMBL2364335
69195880 88563 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(C)c1 10.6019/CHEMBL2364335
CHEMBL2364466 88563 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(C)c1 10.6019/CHEMBL2364335
11518463 88566 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1cc(-c2cc(C)cs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364469 88566 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1cc(-c2cc(C)cs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
69195024 88590 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 3 6 4.2 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364492 88590 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 3 6 4.2 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
44390922 121619 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1cccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL359686 121619 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1cccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
23631026 166885 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelinAgonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelin
ChEMBL 443 5 1 5 5.3 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1CC1CCCNC1 10.1021/jm070071+
CHEMBL429817 166885 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelinAgonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelin
ChEMBL 443 5 1 5 5.3 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1CC1CCCNC1 10.1021/jm070071+
CHEMBL2170779 207611 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Ser123:Ala mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Ser123:Ala mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44447842 94564 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cc(Cl)cc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254972 94564 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cc(Cl)cc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44579804 186472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL491220 186472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145948708 166924 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299606 166924 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
121879 2195 19 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
5868 2195 19 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
CHEMBL308716 2195 19 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
44268996 165899 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL427806 165899 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2)C1 10.1016/s0960-894x(97)10199-8
122178180 120738 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578009 120738 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
44579959 183680 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL483865 183680 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
44454117 155004 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155004 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
162677361 182917 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4799766 182917 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170700 207605 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(C(C)(C)C)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44444570 154218 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 456 5 1 7 3.0 COc1cc2c(cc1N1CCNCC1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL400125 154218 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 456 5 1 7 3.0 COc1cc2c(cc1N1CCNCC1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156017532 177324 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177324 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11662746 97351 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 467 7 2 6 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL271947 97351 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 467 7 2 6 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
122178180 120738 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578009 120738 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578007 210004 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm501702q
16750162 88436 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 474 6 2 7 3.8 COc1ncc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364341 88436 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 474 6 2 7 3.8 COc1ncc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)c(F)c1 10.6019/CHEMBL2364335
11568467 88446 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364351 88446 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197136 88547 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2ccccc2F)s1 10.6019/CHEMBL2364335
CHEMBL2364450 88547 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2ccccc2F)s1 10.6019/CHEMBL2364335
69195304 88561 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 4 2 4 3.9 Cc1cc(S(=O)(=O)Nc2cc(N3C[C@H](C)N[C@H](C)C3)ccc2F)ccc1Br 10.6019/CHEMBL2364335
CHEMBL2364464 88561 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 4 2 4 3.9 Cc1cc(S(=O)(=O)Nc2cc(N3C[C@H](C)N[C@H](C)C3)ccc2F)ccc1Br 10.6019/CHEMBL2364335
145949880 162229 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162229 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
16114099 136687 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375103 136687 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44269018 96886 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc32)C1 10.1016/s0960-894x(97)10199-8
CHEMBL269447 96886 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc32)C1 10.1016/s0960-894x(97)10199-8
145949880 162229 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162229 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
156015598 176993 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
CHEMBL4640573 176993 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
44452827 94969 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 7 3.7 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ccc2C#N)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL257019 94969 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 7 3.7 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ccc2C#N)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
46882582 5663 0 None -125 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 466 5 2 5 3.9 CC1(C)CCc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc2O1 10.1016/j.bmcl.2009.09.027
CHEMBL1078490 5663 0 None -125 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 466 5 2 5 3.9 CC1(C)CCc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc2O1 10.1016/j.bmcl.2009.09.027
145988647 166508 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4289530 166508 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44454367 94804 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 94804 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
16113691 136183 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
CHEMBL374073 136183 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
16113691 136183 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL374073 136183 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
22867380 29192 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 3 3.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL13841 29192 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 3 3.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
2098 3625 31 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
36511 3625 31 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
3805 3625 31 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
3835 3625 31 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
CHEMBL235363 3625 31 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
155561671 175081 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4581511 175081 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44434073 89156 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL237507 89156 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
145981794 166132 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4282394 166132 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56926173 68655 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm1012374
CHEMBL1923501 68655 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm1012374
44301389 11155 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179118 11155 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL61292 11155 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
156015598 176993 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
CHEMBL4640573 176993 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
156017532 177324 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177324 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10100708 11914 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183387 11914 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL294408 11914 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
44579756 186231 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489370 186231 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145958487 161623 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
CHEMBL4162545 161623 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
156016840 177047 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4641215 177047 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL2170779 207611 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
71453489 207613 13 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
10209618 63154 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 11 1 5 5.4 CC(=O)c1ccccc1C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL179978 63154 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 11 1 5 5.4 CC(=O)c1ccccc1C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391041 63975 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 591 11 1 6 5.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181123 63975 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 591 11 1 6 5.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10600702 140792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL383526 140792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10600702 140792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL383526 140792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
9868878 96081 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 460 14 4 9 -0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(N)=O 10.1016/j.bmcl.2008.03.059
CHEMBL262884 96081 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 460 14 4 9 -0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(N)=O 10.1016/j.bmcl.2008.03.059
11306502 63296 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63296 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888395 63559 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 10 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180540 63559 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 10 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
156021942 177639 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 177639 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16113248 78739 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113328 78739 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
23730342 89458 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 511 13 4 10 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCc1cccc(O)c1 10.1021/jm7010595
CHEMBL237916 89458 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 511 13 4 10 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCc1cccc(O)c1 10.1021/jm7010595
145958487 161623 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
CHEMBL4162545 161623 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
156010733 176496 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 176496 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156013130 176918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 176918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156016840 177047 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4641215 177047 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156021942 177639 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 177639 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44570920 183341 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481408 183341 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
44571005 183455 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 4 1 5 2.6 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CCCNCC3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL482204 183455 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 4 1 5 2.6 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CCCNCC3)cc2)o1 10.1016/j.bmcl.2008.12.042
11539144 88451 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
CHEMBL2364356 88451 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
69197315 88467 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364372 88467 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11683663 88493 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364398 88493 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1 10.6019/CHEMBL2364335
11583902 88534 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364437 88534 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1F 10.6019/CHEMBL2364335
69198030 88539 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364442 88539 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69197149 88551 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)c(C)c1 10.6019/CHEMBL2364335
CHEMBL2364454 88551 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)c(C)c1 10.6019/CHEMBL2364335
69196669 88576 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)nc1 10.6019/CHEMBL2364335
CHEMBL2364478 88576 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)nc1 10.6019/CHEMBL2364335
10032659 11931 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183505 11931 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL301259 11931 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
44450137 95841 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 465 12 3 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)Nc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL261234 95841 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 465 12 3 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)Nc1ccccc1 10.1016/j.bmcl.2008.03.059
127046472 139151 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798056 139151 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127046472 139151 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798056 139151 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
145988286 166642 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4291718 166642 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL3578007 210004 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm501702q
CHEMBL61663 214052 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/s0960-894x(01)00324-9
24180592 96552 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 96552 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
162663868 181396 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780408 181396 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
145986080 165888 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4277793 165888 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
168274297 189975 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 299 6 1 1 5.3 CCCCCCCc1cc(=O)c2cc(C(C)(C)C)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5180310 189975 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 299 6 1 1 5.3 CCCCCCCc1cc(=O)c2cc(C(C)(C)C)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
127047523 139520 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3800422 139520 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
44434118 147634 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 467 14 3 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL393570 147634 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 467 14 3 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
44446187 94171 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252255 94171 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
145959787 161723 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
155557019 174005 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174005 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
56926893 68706 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
CHEMBL1923637 68706 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
44437963 200398 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
CHEMBL608826 200398 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
44437963 200398 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
CHEMBL608826 200398 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
44579881 186244 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL489402 186244 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
24180646 147638 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 147638 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
24180646 147638 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 147638 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
145959787 161723 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
46882520 5764 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
CHEMBL1079311 5764 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
46882458 5886 0 None -31 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1080046 5886 0 None -31 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL3578016 210010 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
59007057 88450 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 6 2.8 COc1ccc(NS(=O)(=O)c2ccc(N3CCCC3=O)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364355 88450 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 6 2.8 COc1ccc(NS(=O)(=O)c2ccc(N3CCCC3=O)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11597905 88504 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364409 88504 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198135 88535 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364438 88535 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)c(F)c1 10.6019/CHEMBL2364335
11711997 88552 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 446 5 2 7 2.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)OCCN2C 10.6019/CHEMBL2364335
CHEMBL2364455 88552 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 446 5 2 7 2.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)OCCN2C 10.6019/CHEMBL2364335
44452778 159219 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 6 2 7 3.5 C[C@H]1CN(c2ccc(C(=O)N(C)C)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL410527 159219 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 6 2 7 3.5 C[C@H]1CN(c2ccc(C(=O)N(C)C)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
10437444 112370 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 546 11 2 4 3.8 CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL330989 112370 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 546 11 2 4 3.8 CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
24969603 68697 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
CHEMBL1923627 68697 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
162649450 179464 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4747770 179464 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
156013130 176918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 176918 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44450100 160096 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL411330 160096 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCO)c1 10.1016/j.bmcl.2008.03.059
44411720 10195 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161826 10195 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
44411902 10199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161831 10199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
44411720 10195 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161826 10195 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
44411902 10199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161831 10199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
162656896 180268 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4757313 180268 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
44436883 145608 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
CHEMBL391980 145608 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
156010733 176496 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 176496 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10745674 167380 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL431668 167380 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44579776 192638 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL523795 192638 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
127048061 139193 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798337 139193 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
23730340 89297 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 504 15 4 10 0.4 CC(=O)NCCCCNC(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
CHEMBL237700 89297 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 504 15 4 10 0.4 CC(=O)NCCCCNC(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
56926175 68656 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923504 68656 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
145992835 166270 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4285075 166270 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56925343 68709 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923640 68709 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
145986870 166576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4290627 166576 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44434054 88860 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2cccc(NS(C)(=O)=O)c2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL236857 88860 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2cccc(NS(C)(=O)=O)c2)n1 10.1016/j.bmcl.2007.07.099
44446178 154572 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL402023 154572 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3578016 210010 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
162648837 179248 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745116 179248 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
44391024 63939 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 527 11 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180992 63939 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 527 11 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10745674 167380 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL431668 167380 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391021 19238 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 569 12 1 5 5.3 CC(=O)C(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL129637 19238 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 569 12 1 5 5.3 CC(=O)C(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL2170696 207601 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
23730343 89459 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 12 3 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NC[C@H]1CCCO1 10.1021/jm7010595
CHEMBL237917 89459 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 12 3 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NC[C@H]1CCCO1 10.1021/jm7010595
22888359 63570 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 520 10 1 6 4.8 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C#N)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180591 63570 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 520 10 1 6 4.8 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C#N)C(C)C 10.1016/j.bmcl.2005.02.040
16114514 78733 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
CHEMBL2113322 78733 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
44579843 184160 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL485092 184160 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44579643 186179 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 338 7 1 3 3.2 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488971 186179 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 338 7 1 3 3.2 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579822 191916 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL520953 191916 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
44579755 186350 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 8 1 3 3.6 CCC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490186 186350 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 8 1 3 3.6 CCC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44580032 186242 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 363 7 1 4 3.3 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489398 186242 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 363 7 1 4 3.3 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
145991945 166251 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4284715 166251 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
145992253 166364 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4286849 166364 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL2170702 207607 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
145993313 166328 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286101 166328 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
16114008 84408 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223532 84408 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL501261 212354 19 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.8b01644
9848305 144907 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccc(NS(C)(=O)=O)cc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL391429 144907 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccc(NS(C)(=O)=O)cc2)n1 10.1016/j.bmcl.2007.07.099
44434050 144905 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL391428 144905 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL3578015 210009 0 None -33 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL369482 210406 0 None - 0 Rat 8.0 pED50 = 8 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cn1ccnc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/S0960-894X(01)80239-0
44269087 97762 0 None - 1 Rat 6.7 pED50 = 6.7 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL 553 10 4 7 3.2 CC(C)(NCCCO)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/S0960-894X(01)80239-0
CHEMBL274341 97762 0 None - 1 Rat 6.7 pED50 = 6.7 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL 553 10 4 7 3.2 CC(C)(NCCCO)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/S0960-894X(01)80239-0
70691550 72838 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 572 8 2 5 5.1 Cc1cc(F)ccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011825 72838 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 572 8 2 5 5.1 Cc1cc(F)ccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
16114292 96473 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 96473 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL509976 213794 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
25260901 112968 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319405 112968 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
71456897 81424 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164507 81424 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
70691551 72839 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.3 Cc1cccc(C)c1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011826 72839 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.3 Cc1cccc(C)c1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
25261382 112929 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Partial agonist activity at GHS-R1a (unknown origin)Partial agonist activity at GHS-R1a (unknown origin)
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319215 112929 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Partial agonist activity at GHS-R1a (unknown origin)Partial agonist activity at GHS-R1a (unknown origin)
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
11431274 76976 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL208424 76976 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11577349 64885 1 None - 1 Human 8.0 pIC50 = 8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182655 64885 1 None - 1 Human 8.0 pIC50 = 8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
11351838 77282 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 8 4 6 4.9 CC(NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1)c1ccccc1 10.1021/jm060461g
CHEMBL208842 77282 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 8 4 6 4.9 CC(NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1)c1ccccc1 10.1021/jm060461g
11712151 75625 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205470 75625 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
11713497 122708 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL361349 122708 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
44409757 140780 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 506 8 3 8 4.1 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383454 140780 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 506 8 3 8 4.1 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2006.01.012
127046807 139397 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 139397 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
3676358 5444 4 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 409 3 1 2 4.4 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
CHEMBL1076586 5444 4 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 409 3 1 2 4.4 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
122182047 121475 0 None -67 2 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121475 0 None -67 2 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
122178603 120812 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 120812 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
11649248 66322 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185399 66322 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
44395020 123501 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL363021 123501 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
44389262 121505 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
CHEMBL359506 121505 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
145993628 166826 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 483 4 1 2 6.1 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4295148 166826 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 483 4 1 2 6.1 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11211892 79791 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL213703 79791 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
122178611 120821 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 120821 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
11846624 77548 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209443 77548 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
11846463 138699 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL378909 138699 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
11430392 76356 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
CHEMBL206588 76356 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
57797614 72830 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 558 8 2 5 4.8 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011817 72830 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 558 8 2 5 4.8 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
44409801 76365 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 5 3 7 3.6 CC(C)(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206638 76365 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 5 3 7 3.6 CC(C)(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11523411 75189 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
CHEMBL204511 75189 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
11537800 75201 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
CHEMBL204564 75201 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
71453392 81421 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164504 81421 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
71456910 81475 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164823 81475 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
71460578 81482 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164830 81482 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
122178612 120822 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 120822 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL507636 212652 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
56942387 139119 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 139119 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145991822 166395 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 6.8 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4287267 166395 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 6.8 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11676995 65816 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184258 65816 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
127048038 139429 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 139429 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
71458746 81411 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1ccc2c(c1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
CHEMBL2164493 81411 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1ccc2c(c1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
145992142 166207 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4283858 166207 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
71460565 81413 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2012.07.018
CHEMBL2164495 81413 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2012.07.018
11538533 74636 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203280 74636 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
46880462 6175 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081648 6175 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
70693641 72841 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 538 8 2 5 4.4 O=C1CN([C@@H](C(=O)NC2CCN(Cc3ccccc3)CC2)C2CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
CHEMBL2011828 72841 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 538 8 2 5 4.4 O=C1CN([C@@H](C(=O)NC2CCN(Cc3ccccc3)CC2)C2CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
44409756 76399 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206820 76399 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46865987 7501 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1087908 7501 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880772 5819 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079624 5819 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11538534 74649 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203373 74649 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
145986870 166576 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4290627 166576 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
127046806 139390 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 139390 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
122178613 120823 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 120823 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
145981196 165972 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4279344 165972 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
46880814 6285 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 413 3 2 3 3.5 C[C@H]1CN(C(=O)c2ccc(-c3cn[nH]c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082190 6285 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 413 3 2 3 3.5 C[C@H]1CN(C(=O)c2ccc(-c3cn[nH]c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178616 120825 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 120825 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
145986461 166649 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4291926 166649 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71451551 81425 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164508 81425 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
46880727 6053 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080939 6053 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122182190 121482 0 None -8 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121482 0 None -8 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44409840 75974 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc43)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205896 75974 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc43)cc2)cc1 10.1016/j.bmcl.2006.01.012
127047362 139176 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 139176 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145989916 166182 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 491 5 2 4 5.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(O)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4283454 166182 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 491 5 2 4 5.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(O)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
127048038 139429 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 139429 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
46880673 6013 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080755 6013 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11455251 160755 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL412362 160755 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409611 74323 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 463 6 3 7 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC4CCC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203019 74323 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 463 6 3 7 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC4CCC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
11221946 140302 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL381942 140302 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
44409839 75890 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205847 75890 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
71460576 81479 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3c(Cl)cc(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164828 81479 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3c(Cl)cc(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL509976 213794 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
11692087 62648 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178610 62648 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
44409758 75606 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205374 75606 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409661 75628 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 423 6 3 7 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205484 75628 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 423 6 3 7 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880724 6166 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1cc(-c2ccccc2)ccc1C(=O)N1CCN(C(=O)c2ccc3cc[nH]c3c2)[C@@H](C)C1 10.1016/j.bmcl.2010.01.043
CHEMBL1081611 6166 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1cc(-c2ccccc2)ccc1C(=O)N1CCN(C(=O)c2ccc3cc[nH]c3c2)[C@@H](C)C1 10.1016/j.bmcl.2010.01.043
71455105 81478 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 432 4 2 4 2.6 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164827 81478 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 432 4 2 4 2.6 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
11221946 140302 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
CHEMBL381942 140302 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
44410003 75813 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205794 75813 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880811 5906 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3cccnc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080162 5906 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3cccnc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70687379 72836 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1cccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)c1 10.1016/j.bmcl.2012.01.014
CHEMBL2011823 72836 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1cccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)c1 10.1016/j.bmcl.2012.01.014
44394974 66662 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186974 66662 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL3586019 210044 4 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by inositol phosphate turnover assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by inositol phosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
46880567 6295 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3cccc(F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082210 6295 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3cccc(F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71460564 81410 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 488 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(C(C)(C)C)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164492 81410 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 488 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(C(C)(C)C)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
145992854 166302 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4285747 166302 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C2)ncn1 10.1021/acs.jmedchem.8b00794
44394833 126291 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365460 126291 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL509976 213794 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL509976 213794 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL509976 213794 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
127047654 139434 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 139434 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
145993758 166751 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 490 5 2 4 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(N)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294024 166751 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 490 5 2 4 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(N)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
145993528 166753 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294083 166753 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL444131 212171 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None NC(=O)CNC(=O)CNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1074/jbc.m609796200
11476589 75620 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205451 75620 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11329138 64114 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL181350 64114 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1016/j.bmcl.2012.01.014
70681022 72845 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NC(C)(C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011833 72845 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NC(C)(C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL509976 213794 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
122178611 120821 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 120821 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
46880675 6051 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2F)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080927 6051 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2F)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11612155 140465 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL382375 140465 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
328912 62232 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
CHEMBL178266 62232 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
70685218 72833 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3cccc(Cl)c3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011820 72833 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3cccc(Cl)c3)cc2C1=O 10.1016/j.bmcl.2012.01.014
145981794 166132 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4282394 166132 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11649239 65993 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185057 65993 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL501261 212354 19 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
1744826 62654 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178668 62654 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
11282247 165362 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL425048 165362 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11282247 165362 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL425048 165362 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
1744826 62654 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178668 62654 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409831 75331 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 503 6 3 9 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3COc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204776 75331 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 503 6 3 9 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3COc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
145979268 166100 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4281647 166100 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44409678 140673 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382853 140673 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11349789 78348 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211265 78348 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11692087 62648 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178610 62648 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
11677781 124525 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL364430 124525 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
11538533 74636 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
CHEMBL203280 74636 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
11154823 75661 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205660 75661 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
56942244 124664 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 124664 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44409994 75814 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 409 6 3 7 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205796 75814 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 409 6 3 7 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 212441 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44395002 65840 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184368 65840 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
11646276 75566 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL205136 75566 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
127046807 139397 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 139397 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
16113695 136490 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374643 136490 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
145987684 166713 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4293331 166713 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
122178602 120811 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 120811 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
70681020 72842 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011829 72842 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
56942098 124660 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 124660 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942242 124662 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 124662 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
127046956 139414 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 139414 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
66788278 124659 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 124659 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046956 139414 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 139414 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
57797640 72864 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 510 9 1 3 7.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011892 72864 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 510 9 1 3 7.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
46880628 5940 0 None 4 2 Rat 8.7 pIC50 = 8.7 Functional
Inhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayInhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080389 5940 0 None 4 2 Rat 8.7 pIC50 = 8.7 Functional
Inhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayInhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178606 120815 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 120815 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
46880629 5966 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 457 3 1 2 5.5 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080556 5966 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 457 3 1 2 5.5 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178606 120815 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 120815 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
70681021 72844 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.2 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011832 72844 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.2 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
70691552 72846 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)C2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011834 72846 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)C2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
44576247 212441 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
122178607 120817 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 120817 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
46880631 6043 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1080907 6043 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
46880726 6052 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080938 6052 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70689441 72863 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011891 72863 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
145988582 166727 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 555 4 1 2 7.4 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#C[Si](C)(C)C)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4293608 166727 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 555 4 1 2 7.4 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#C[Si](C)(C)C)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
122178610 120820 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 120820 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
44409666 75519 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 437 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204897 75519 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 437 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 212441 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL500703 212339 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
44409802 76376 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206687 76376 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178613 120823 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 120823 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
71458747 81412 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164494 81412 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
56942244 124664 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 124664 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
11537683 75161 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL204352 75161 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
71449740 81414 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 4 2 4 3.5 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2012.07.018
CHEMBL2164497 81414 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 4 2 4 3.5 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2012.07.018
122178601 120810 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 120810 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
11337482 76272 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL206399 76272 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
122178614 120824 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 120824 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
44389168 64527 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL182154 64527 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
145991389 166440 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 6 1 6 6.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4288108 166440 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 6 1 6 6.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
145990051 166391 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 499 5 1 2 7.0 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4287218 166391 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 499 5 1 2 7.0 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44410012 137858 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377305 137858 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
71462272 81419 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 4.6 CN(C)C1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164502 81419 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 4.6 CN(C)C1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
71451563 81484 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164832 81484 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
145988286 166642 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4291718 166642 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
46880813 6284 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 4 4.4 Cc1noc(C)c1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1082189 6284 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 4 4.4 Cc1noc(C)c1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
44409761 75498 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204880 75498 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11846625 77516 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209394 77516 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
122178610 120820 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 120820 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
46880461 6143 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 439 4 1 3 4.4 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)CC3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081483 6143 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 439 4 1 3 4.4 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)CC3)cc2)c1 10.1016/j.bmcl.2010.01.043
71453391 81420 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164503 81420 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
1221269 121507 12 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359530 121507 12 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389151 62161 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL178138 62161 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
71451564 81486 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
CHEMBL2164834 81486 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
71449753 81476 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 465 4 2 3 4.7 CC1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164825 81476 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 465 4 2 3 4.7 CC1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
44409871 75031 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203948 75031 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880569 6097 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1081212 6097 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
70693640 72835 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011822 72835 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL449590 212202 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
44576247 212441 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
145994299 166831 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 5 1 4 6.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4295212 166831 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 5 1 4 6.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71460577 81480 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)c(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164829 81480 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)c(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
16113902 137138 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL375859 137138 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
71462274 81423 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 3.8 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1=O 10.1016/j.bmc.2012.07.018
CHEMBL2164506 81423 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 3.8 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1=O 10.1016/j.bmc.2012.07.018
CHEMBL509976 213794 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
70683143 72834 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(Cl)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011821 72834 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(Cl)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
46880495 6277 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082162 6277 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
11697618 62255 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178289 62255 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145988557 166696 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4292914 166696 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44409771 140709 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383073 140709 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
145980333 166017 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4280040 166017 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11329138 64114 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium levelAntagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium level
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
CHEMBL181350 64114 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium levelAntagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium level
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
44576247 212441 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11568561 168976 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
CHEMBL443560 168976 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
145991945 166251 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4284715 166251 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
44394982 65792 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cellsAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184093 65792 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cellsAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
66788278 124659 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 124659 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942099 124661 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 124661 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942243 124663 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 124663 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
127045858 139319 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 139319 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
70681018 72832 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011819 72832 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
70685225 72866 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 576 8 2 5 5.0 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011894 72866 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 576 8 2 5 5.0 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
11410373 137993 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
CHEMBL377514 137993 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
11339816 75639 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205521 75639 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145992253 166364 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4286849 166364 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11503585 64858 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182542 64858 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
44409762 75518 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204884 75518 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180026 121060 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium responseAntagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium response
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 121060 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium responseAntagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium response
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
46880846 7516 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1088038 7516 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
44389248 121641 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359714 121641 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
70695749 72848 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 562 9 2 6 4.3 CC(C)[C@H](C(=O)N1CCC(NCCC2CCOCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011836 72848 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 562 9 2 6 4.3 CC(C)[C@H](C(=O)N1CCC(NCCC2CCOCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
122178614 120824 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 120824 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
70695748 72840 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 498 7 2 5 3.7 O=C1CN(CC(=O)NC2CCN(Cc3ccccc3)CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
CHEMBL2011827 72840 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 498 7 2 5 3.7 O=C1CN(CC(=O)NC2CCN(Cc3ccccc3)CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
145981687 166013 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4279987 166013 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11508639 76167 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL206091 76167 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
44409683 75891 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205848 75891 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11626181 123849 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363896 123849 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
11690097 76304 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL206446 76304 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
44409775 75657 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205605 75657 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 212441 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11655355 74057 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL202642 74057 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
127047654 139434 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 139434 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
16113799 168137 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL436849 168137 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
145986080 165888 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4277793 165888 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56942385 124665 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 124665 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
46880771 5818 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 448 3 1 4 4.4 C[C@H]1CN(C(=O)c2csc(-c3ccccc3F)n2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079623 5818 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 448 3 1 4 4.4 C[C@H]1CN(C(=O)c2csc(-c3ccccc3F)n2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11654867 75833 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205833 75833 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
122178600 120809 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 120809 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
46880844 7500 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 432 3 1 4 3.0 C[C@H]1CN(C(=O)c2ccc(N3CCOCC3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1087907 7500 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 432 3 1 4 3.0 C[C@H]1CN(C(=O)c2ccc(N3CCOCC3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11248021 138712 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 454 8 4 6 4.3 Nc1nc(N)c(-c2ccc(NC(=O)NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378989 138712 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 454 8 4 6 4.3 Nc1nc(N)c(-c2ccc(NC(=O)NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122182189 121481 0 None -7 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121481 0 None -7 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
44409865 140174 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3Cc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381759 140174 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3Cc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11751384 140962 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL384524 140962 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409679 75142 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204322 75142 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409868 76374 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206673 76374 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409667 75601 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 451 6 3 7 4.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205294 75601 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 451 6 3 7 4.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 212441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
56942388 139400 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 139400 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
11166495 75184 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL204474 75184 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
145994050 166780 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4294493 166780 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11538533 74636 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203280 74636 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880770 5817 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cn2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079622 5817 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cn2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71453390 81417 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164500 81417 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
44409763 140821 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 6 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3Cc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383757 140821 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 6 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3Cc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409989 165262 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL424860 165262 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44410008 140707 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383058 140707 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11178309 79476 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL212415 79476 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11517629 167764 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL434330 167764 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
127047655 139071 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 139071 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046957 139164 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 139164 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
127045858 139319 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 139319 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
56942098 124660 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 124660 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046957 139164 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 139164 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
46880630 6006 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3C(F)(F)F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080735 6006 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3C(F)(F)F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70685219 72847 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 9 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NCCC2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011835 72847 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 9 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NCCC2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
16113245 120807 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 120807 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
122178607 120817 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 120817 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
11452801 138755 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL379191 138755 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
46882763 5537 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilizationAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilization
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077617 5537 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilizationAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilization
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44409776 76775 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207754 76775 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145991797 166352 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 613 5 1 6 6.5 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)NCc4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286597 166352 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 613 5 1 6 6.5 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)NCc4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
122178616 120825 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 120825 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
11430583 79792 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL213704 79792 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL509976 213794 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
11669486 64268 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL181736 64268 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
44409946 139272 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 514 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL379887 139272 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 514 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
127046806 139390 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 139390 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
122178600 120809 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 120809 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
11605333 76357 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
CHEMBL206589 76357 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
46880845 7515 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 460 3 1 3 4.5 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1088037 7515 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 460 3 1 3 4.5 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880773 6115 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccn3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081301 6115 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccn3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178604 120813 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 120813 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
56942387 139119 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 139119 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44576247 212441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11683469 76338 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
CHEMBL206486 76338 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
44389216 123323 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
CHEMBL362595 123323 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
145979819 165909 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4278185 165909 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
46880498 5903 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080155 5903 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71462273 81422 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164505 81422 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
71453404 81477 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164826 81477 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
44389283 62601 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178494 62601 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
11179347 76985 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL208477 76985 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44409764 76781 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207792 76781 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11606121 64230 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
CHEMBL181584 64230 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
11539587 66727 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187271 66727 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL3586019 210044 4 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Inverse agonist activity at rat ghrelin receptor by inositol phosphate turnover assayInverse agonist activity at rat ghrelin receptor by inositol phosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
122178608 120818 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 120818 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
44409821 75669 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205711 75669 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11340044 140791 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL383522 140791 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
70683149 72861 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 504 8 2 5 3.9 CC(C)[C@H](C(=O)N1CCC(NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011887 72861 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 504 8 2 5 3.9 CC(C)[C@H](C(=O)N1CCC(NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
71452183 83102 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assayAntagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assay
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
CHEMBL2203623 83102 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assayAntagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assay
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
122178602 120811 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 120811 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
11582836 62569 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178463 62569 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389192 168070 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL436275 168070 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
71455106 81487 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 442 5 2 5 2.2 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(C)cc32)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164835 81487 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 442 5 2 5 2.2 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(C)cc32)cc1 10.1016/j.bmc.2012.07.018
44409998 137994 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377515 137994 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145984632 165827 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4276775 165827 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
10415364 126233 0 None -5 3 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126233 0 None -5 3 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
15949382 74484 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203158 74484 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
145993313 166328 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286101 166328 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11605822 123856 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363930 123856 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
11154001 79463 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 406 7 4 6 3.6 CC(C)NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL212354 79463 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 406 7 4 6 3.6 CC(C)NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
44394930 65985 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185028 65985 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
11699004 65856 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184429 65856 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
11618705 166374 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL428698 166374 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
44409785 75435 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204852 75435 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409990 76149 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205995 76149 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145992125 166186 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4283504 166186 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
46880568 6296 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082211 6296 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70687383 72862 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.6 CC(C)[C@H](C[C@H]1CC[C@@H](NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011890 72862 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.6 CC(C)[C@H](C[C@H]1CC[C@@H](NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
16113245 120807 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 120807 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL509976 213794 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
57422817 112937 13 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319223 112937 13 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
11190594 75617 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205445 75617 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
56942385 124665 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 124665 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44576247 212441 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
16113904 136499 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374655 136499 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
44389215 62734 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178838 62734 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44576247 212441 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44409809 74700 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203578 74700 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113468 141256 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL386218 141256 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
11531313 62160 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178137 62160 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389167 123327 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL362612 123327 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
46880674 6050 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccc(F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080926 6050 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccc(F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71455085 81418 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 4 2 4 4.3 CN1CCCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164501 81418 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 4 2 4 4.3 CN1CCCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
46880463 6176 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081649 6176 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
46880812 5929 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 430 3 1 4 4.3 C[C@H]1CN(C(=O)c2ccc(-c3cncs3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080320 5929 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 430 3 1 4 4.3 C[C@H]1CN(C(=O)c2ccc(-c3cncs3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880497 6279 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 O=C(c1ccc(-c2ccccc2)cc1)N1CCCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
CHEMBL1082164 6279 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 O=C(c1ccc(-c2ccccc2)cc1)N1CCCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
44409770 140824 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383766 140824 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178604 120813 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 120813 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
46880496 6278 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082163 6278 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL502208 212369 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1074/jbc.m609796200
145980382 166079 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4281310 166079 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44389186 64269 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL181739 64269 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409864 75133 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204266 75133 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409975 75423 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204835 75423 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409455 75600 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
CHEMBL205286 75600 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
11441554 218 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
5871 218 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
CHEMBL212761 218 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
11340329 79177 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 9 4 6 4.4 Nc1nc(N)c(-c2ccc(NC(=O)NCCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211454 79177 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 9 4 6 4.4 Nc1nc(N)c(-c2ccc(NC(=O)NCCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122178605 120814 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 120814 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
127047655 139071 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 139071 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
46880672 6104 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1081254 6104 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)cc1 10.1016/j.bmcl.2010.01.043
66601728 81415 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164499 81415 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
70689440 72831 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL2011818 72831 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
70693644 72865 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 496 9 1 3 6.7 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011893 72865 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 496 9 1 3 6.7 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
70695747 72829 0 None 1 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 72829 0 None 1 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
11225576 165473 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL425594 165473 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11225576 165473 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL425594 165473 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
122178608 120818 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 120818 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
122178609 120819 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 120819 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
56942388 139400 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 139400 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942535 139218 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 139218 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
11176805 76966 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
CHEMBL208374 76966 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
71453405 81485 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 462 5 2 5 2.6 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(Cl)cc32)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164833 81485 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 462 5 2 5 2.6 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(Cl)cc32)cc1 10.1016/j.bmc.2012.07.018
44394913 126639 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365721 126639 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
44409832 76042 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205955 76042 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
25190383 81483 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164831 81483 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
122178615 120777 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 120777 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
44410013 76685 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207268 76685 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44389243 64237 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
CHEMBL181619 64237 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
753168 122710 33 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL361366 122710 33 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
46880566 6294 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082209 6294 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178603 120812 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 120812 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
44409979 140016 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381159 140016 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11256439 75014 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
CHEMBL203843 75014 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
11655578 169455 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL444277 169455 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
70681019 72837 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL2011824 72837 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
122178612 120822 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 120822 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
11617435 75629 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL205486 75629 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
145988647 166508 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4289530 166508 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11663710 123935 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363995 123935 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
56942099 124661 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 124661 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942242 124662 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 124662 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
11663710 123935 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL363995 123935 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2012.01.014
70695747 72829 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 72829 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
70687380 72843 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011831 72843 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
122178605 120814 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 120814 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
145988894 166580 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4290680 166580 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
16203569 141189 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL385803 141189 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
145981343 166145 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4282719 166145 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL509976 213794 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
122178615 120777 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 120777 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
44409810 140356 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 9 3 9 2.8 CCOC(=O)CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382138 140356 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 9 3 9 2.8 CCOC(=O)CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113124 120808 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581032 120808 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
44576247 212441 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44409536 75143 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL204325 75143 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145992835 166270 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4285075 166270 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11327400 75007 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL203782 75007 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11539588 66564 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186540 66564 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
16113796 84244 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL222518 84244 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
11442040 78126 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 440 7 4 6 4.7 Nc1nc(N)c(-c2ccc(NC(=O)Nc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211211 78126 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 440 7 4 6 4.7 Nc1nc(N)c(-c2ccc(NC(=O)Nc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122178601 120810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 120810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
56942243 124663 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 124663 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
46880725 6167 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 455 3 1 2 5.3 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1F 10.1016/j.bmcl.2010.01.043
CHEMBL1081612 6167 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 455 3 1 2 5.3 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1F 10.1016/j.bmcl.2010.01.043
122178609 120819 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 120819 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
11454617 140775 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
CHEMBL383411 140775 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
46880628 5940 0 None -4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080389 5940 0 None -4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
44409684 140341 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382033 140341 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409672 139944 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL380971 139944 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409673 76382 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL206741 76382 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
11453509 75810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205784 75810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
127047362 139176 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 139176 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
56942535 139218 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 139218 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145990956 166457 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 4 1 2 6.6 C[C@H](NC(=O)N(C)C1CCN(C2CCc3ccccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4288441 166457 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 4 1 2 6.6 C[C@H](NC(=O)N(C)C1CCN(C2CCc3ccccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44394947 168646 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL440939 168646 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
44410007 76059 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205963 76059 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11583811 75619 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205450 75619 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11576960 66764 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187427 66764 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
11281346 75650 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205568 75650 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL499371 212314 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC(N)=O)C(N)=O 10.1074/jbc.m609796200
155540883 172378 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172378 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155540883 172378 0 None - 1 Human 8.0 pKd = 8.0 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172378 0 None - 1 Human 8.0 pKd = 8.0 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155557019 174005 0 None - 1 Human 7.5 pKd = 7.5 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174005 0 None - 1 Human 7.5 pKd = 7.5 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155557019 174005 0 None - 1 Human 7.1 pKd = 7.1 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174005 0 None - 1 Human 7.1 pKd = 7.1 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57399248 68687 0 None - 1 Human 9.0 pKi = 9 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923617 68687 0 None - 1 Human 9.0 pKi = 9 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
71452183 83102 0 None - 1 Human 7.0 pKi = 7 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
CHEMBL2203623 83102 0 None - 1 Human 7.0 pKi = 7 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
44454117 155004 0 None - 1 Human 7.9 pKi = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155004 0 None - 1 Human 7.9 pKi = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
44454060 154781 0 None - 1 Human 5.9 pKi = 5.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 154781 0 None - 1 Human 5.9 pKi = 5.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454367 94804 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 94804 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
44454338 97373 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL272085 97373 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44434080 89467 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL237933 89467 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454302 158821 0 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL410060 158821 0 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
44454092 97187 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97187 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454432 154707 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 154707 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
9950632 88264 0 None - 1 Human 5.5 pKi = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
CHEMBL236038 88264 0 None - 1 Human 5.5 pKi = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
44454399 154588 0 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL402086 154588 0 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
44454432 154707 0 None - 1 Human 5.4 pKi = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 154707 0 None - 1 Human 5.4 pKi = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
25022640 97339 0 None - 1 Human 7.4 pKi = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL271876 97339 0 None - 1 Human 7.4 pKi = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454092 97187 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97187 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454303 97107 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL270666 97107 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
44454304 97141 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL270876 97141 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
56926461 68679 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923609 68679 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
44454398 97136 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL270851 97136 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
44454060 154781 0 None - 1 Human 7.2 pKi = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 154781 0 None - 1 Human 7.2 pKi = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454367 94804 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 94804 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
44454337 155051 0 None - 1 Human 8.1 pKi = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL404545 155051 0 None - 1 Human 8.1 pKi = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44454117 155004 0 None - 1 Human 6.1 pKi = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155004 0 None - 1 Human 6.1 pKi = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
1099 1749 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Measuring ghrelin-induced GHSR activation detected by β-arrestin recruitment in cells stably expressing hGHSR.Measuring ghrelin-induced GHSR activation detected by β-arrestin recruitment in cells stably expressing hGHSR.
Guide to Pharmacology None None None None 29233536
121879 2195 19 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5868 2195 19 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
CHEMBL308716 2195 19 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5869 4005 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
121879 2195 19 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
5868 2195 19 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
CHEMBL308716 2195 19 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
1099 1749 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10628755
1099 1749 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
121879 2195 19 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5868 2195 19 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
CHEMBL308716 2195 19 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
1093 1756 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1756 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1756 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
178024 1932 30 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
178024 1932 30 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
5867 1932 30 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
5867 1932 30 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
CHEMBL13817 1932 30 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
CHEMBL13817 1932 30 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
1099 1749 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1749 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
5866 3554 3 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
9804743 3554 3 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
CHEMBL360227 3554 3 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
9734 2289 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
IC<sub>50</sub> for LEAP2 antagonism of GHSR activation in the presence of ghrelin.IC<sub>50</sub> for LEAP2 antagonism of GHSR activation in the presence of ghrelin.
Guide to Pharmacology None None None None 29233536
11441554 218 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
5871 218 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
CHEMBL212761 218 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
5872 2084 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 10 3 8 5.4 COc1ccc(c(c1)OC)n1c(nnc1n1cc(c2c1cccc2)CC)[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H]1CCCN1 17927165
74015851 2084 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 10 3 8 5.4 COc1ccc(c(c1)OC)n1c(nnc1n1cc(c2c1cccc2)CC)[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H]1CCCN1 17927165
25124566 1836 6 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
5870 1836 6 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
CHEMBL3358452 1836 6 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
5866 3554 3 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
9804743 3554 3 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
CHEMBL360227 3554 3 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
25124566 1836 6 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740
5870 1836 6 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740
CHEMBL3358452 1836 6 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740




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
178024 1932 30 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
5867 1932 30 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
CHEMBL13817 1932 30 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
22867441 10203 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL1161835 10203 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
67457995 91387 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@H](O)c1ccccc12 10.1016/j.bmc.2013.06.006
CHEMBL2413152 91387 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@H](O)c1ccccc12 10.1016/j.bmc.2013.06.006
22867441 10203 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL1161835 10203 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
71716660 85561 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL2304221 85561 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10345516 138732 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
CHEMBL379074 138732 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
71716660 85561 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL2304221 85561 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10345516 138732 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
CHEMBL379074 138732 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
9807597 182425 3 None - 0 Human 9.0 pEC50 = 9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL47938 182425 3 None - 0 Human 9.0 pEC50 = 9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
10323604 10197 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161828 10197 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10323604 10197 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161828 10197 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411920 77510 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL209360 77510 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
162662316 180931 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 542 8 3 6 2.6 CC(C)(N)NC(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CC(S(C)(=O)=O)c1ccccc12 10.1021/acs.jmedchem.0c00829
CHEMBL4765101 180931 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 542 8 3 6 2.6 CC(C)(N)NC(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CC(S(C)(=O)=O)c1ccccc12 10.1021/acs.jmedchem.0c00829
90666017 108799 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assayAgonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assay
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218890 108799 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assayAgonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assay
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44411920 77510 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL209360 77510 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
10625750 167580 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL433087 167580 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10625750 167580 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL433087 167580 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10626337 100742 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
CHEMBL295984 100742 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
44411718 10194 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161825 10194 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44293557 100606 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL294923 100606 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL540001 100606 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
16040587 178794 0 None - 0 Human 7.0 pEC50 = 7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm301653f
CHEMBL473921 178794 0 None - 0 Human 7.0 pEC50 = 7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm301653f
16040587 178794 0 None - 0 Human 7.0 pEC50 = 7 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
CHEMBL473921 178794 0 None - 0 Human 7.0 pEC50 = 7 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
16752689 187774 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1021/jm301653f
CHEMBL501315 187774 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1021/jm301653f
9890375 97805 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL274599 97805 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL558802 97805 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
9890375 97805 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL274599 97805 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL558802 97805 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10026738 162207 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL417182 162207 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL557206 162207 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10026738 162207 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL417182 162207 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL557206 162207 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10745533 139577 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL380096 139577 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10745533 139577 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL380096 139577 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
44411745 10196 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161827 10196 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
10626337 100742 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
CHEMBL295984 100742 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
44411634 10193 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161824 10193 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411634 10193 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161824 10193 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411745 10196 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161827 10196 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411753 10198 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161829 10198 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44411753 10198 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161829 10198 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44293091 187593 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL49884 187593 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
44293091 187593 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL49884 187593 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
46905972 10296 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
CHEMBL1162926 10296 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
15481181 77376 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL209020 77376 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
9810101 98779 12 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL281764 98779 12 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
15481188 140666 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL382844 140666 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL1793862 207175 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm058053k
216208 9620 27 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.0c00829
CHEMBL113313 9620 27 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.0c00829
46905972 10296 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
CHEMBL1162926 10296 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
15481181 77376 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL209020 77376 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
9810101 98779 12 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL281764 98779 12 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
15481188 140666 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL382844 140666 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL1793862 207175 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm058053k
15481185 76893 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL207970 76893 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
15481185 76893 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL207970 76893 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
44411584 10191 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161822 10191 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411584 10191 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161822 10191 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
22862436 10202 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161834 10202 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10602640 137648 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
CHEMBL376970 137648 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
10791616 138993 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL379564 138993 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10029990 168707 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL441360 168707 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
22862436 10202 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161834 10202 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10602640 137648 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
CHEMBL376970 137648 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
10791616 138993 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL379564 138993 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10029990 168707 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL441360 168707 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
44411632 10192 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161823 10192 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411632 10192 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161823 10192 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
23529194 101708 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 525 5 3 3 4.0 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1)NC1CN2CCC1CC2 10.1021/acs.jmedchem.0c00829
CHEMBL302810 101708 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 525 5 3 3 4.0 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1)NC1CN2CCC1CC2 10.1021/acs.jmedchem.0c00829
16041292 183019 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 490 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-n3ccnc3C(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
CHEMBL480219 183019 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 490 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-n3ccnc3C(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
44411913 10201 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161833 10201 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411913 10201 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161833 10201 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411905 10200 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161832 10200 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10506325 100758 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL296104 100758 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
44411905 10200 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161832 10200 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10506325 100758 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL296104 100758 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
10600702 140792 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL383526 140792 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10600702 140792 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL383526 140792 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL335799 209808 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmc.2013.06.006
44411720 10195 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161826 10195 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411902 10199 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161831 10199 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44411720 10195 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161826 10195 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411902 10199 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161831 10199 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44390849 62571 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL178475 62571 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
25227441 112931 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 563 8 2 8 3.9 CCc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319217 112931 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 563 8 2 8 3.9 CCc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL501253 212352 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CCCCCCCBr)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
44582528 192803 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
91935097 192803 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
CHEMBL525994 192803 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
CHEMBL2310891 207740 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
90665845 108771 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 485 5 0 4 6.8 Cc1ccccc1-c1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218645 108771 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 485 5 0 4 6.8 Cc1ccccc1-c1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL500468 212334 0 None - 1 Human 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2005.02.042
57422686 112935 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 600 8 2 9 4.1 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccc5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319221 112935 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 600 8 2 9 4.1 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccc5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL2310888 207738 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O)C(C)C 10.1021/jm0001727
11340044 140791 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL383522 140791 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44336274 108070 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 bindingInhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 binding
ChEMBL 896 22 6 10 2.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CN(S(=O)(=O)CC(=O)NCCCCCCNC(=O)CCCC[C@@H]1SCC3NC(=O)NC31)c1ccccc12 10.1021/jm970342o
CHEMBL320289 108070 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 bindingInhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 binding
ChEMBL 896 22 6 10 2.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CN(S(=O)(=O)CC(=O)NCCCCCCNC(=O)CCCC[C@@H]1SCC3NC(=O)NC31)c1ccccc12 10.1021/jm970342o
122180027 121061 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586033 121061 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
118709502 112960 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319398 112960 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
44390862 63521 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cc(Cl)ccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180349 63521 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cc(Cl)ccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
16133832 211573 15 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL425281 211573 15 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL500468 212334 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/s0960-894x(01)00324-9
90665847 108773 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3ccc(Cl)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218647 108773 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3ccc(Cl)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
122182190 121482 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121482 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
57422687 112936 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 604 8 2 9 3.9 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319222 112936 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 604 8 2 9 3.9 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
16114292 96473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 96473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
16114292 96473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL266063 96473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
11225576 165473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL425594 165473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
122182047 121475 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121475 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
11225576 165473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL425594 165473 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
25260749 112934 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 579 9 2 9 3.7 CCOc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319220 112934 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 579 9 2 9 3.7 CCOc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
57422792 112959 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 635 8 2 10 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(Cl)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319397 112959 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 635 8 2 10 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(Cl)cc4Cl)sc3c2)CC1 10.1021/jm500610n
57422692 112933 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 575 8 2 8 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(C5CC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319219 112933 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 575 8 2 8 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(C5CC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL500468 212334 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm020985q
122182043 121471 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 121471 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
118709506 112970 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 586 5 2 9 4.3 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319407 112970 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 586 5 2 9 4.3 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
178024 1932 30 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
5867 1932 30 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
CHEMBL13817 1932 30 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
11431274 76976 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL208424 76976 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11410373 137993 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
CHEMBL377514 137993 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
44582531 188126 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
91935100 188126 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL504776 188126 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
122182046 121474 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 121474 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
25260745 112963 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 573 10 2 8 5.2 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319400 112963 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 573 10 2 8 5.2 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
122182190 121482 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121482 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
57422768 112942 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c(Cl)c2)n1 10.1021/jm500610n
CHEMBL3319228 112942 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c(Cl)c2)n1 10.1021/jm500610n
16114096 78735 1 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113324 78735 1 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
178024 1932 30 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
5867 1932 30 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
CHEMBL13817 1932 30 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
57422690 112941 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
CHEMBL3319227 112941 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
118709503 112961 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 588 7 2 9 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(ccn5C)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319399 112961 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 588 7 2 9 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(ccn5C)cc4Cl)sc3c2)CC1 10.1021/jm500610n
66788278 124659 0 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645254 124659 0 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
16114292 96473 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
CHEMBL266063 96473 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
44436850 91104 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240509 91104 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
57422793 112958 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 631 9 2 11 3.5 COc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1021/jm500610n
CHEMBL3319396 112958 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 631 9 2 11 3.5 COc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1021/jm500610n
178024 1932 30 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
5867 1932 30 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
CHEMBL13817 1932 30 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
57422688 112939 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319225 112939 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
57785733 112938 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 612 8 2 9 4.4 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-c5ccccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319224 112938 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 612 8 2 9 4.4 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-c5ccccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
16113245 120807 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 120807 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
44445600 154238 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL400175 154238 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL437713 211973 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cells
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm020424z
178024 1932 30 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
5867 1932 30 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL13817 1932 30 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL412799 211268 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(N)=O)C(C)C 10.1021/jm0001727
57422817 112937 13 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319223 112937 13 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
11476589 75620 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205451 75620 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL526723 213911 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
44436857 145111 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL391588 145111 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
90666039 108821 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 8 0 9 4.2 CCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218912 108821 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 8 0 9 4.2 CCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
118709505 112969 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 561 5 2 8 4.4 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319406 112969 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 561 5 2 8 4.4 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL2310887 207737 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCC(CCC)C(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
122180026 121060 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 121060 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
122182043 121471 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 121471 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL2310890 207739 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None C/C=C/C=C/C=C/C(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
44409536 75143 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL204325 75143 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44445595 93954 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL250974 93954 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90665850 108776 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 7 0 7 4.6 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cn(-c4ccc(Cl)cc4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218650 108776 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 7 0 7 4.6 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cn(-c4ccc(Cl)cc4)nc3c2=O)C1 10.1039/C2MD20340E
90665851 108777 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 459 5 0 6 4.8 Cc1ccccc1-c1nc2cn(-c3ccc(F)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218651 108777 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 459 5 0 6 4.8 Cc1ccccc1-c1nc2cn(-c3ccc(F)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
11134880 98959 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL282891 98959 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
5866 3554 3 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
9804743 3554 3 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
CHEMBL360227 3554 3 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
11712151 75625 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205470 75625 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
56942098 124660 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645255 124660 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
25261382 112929 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319215 112929 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
57422789 112943 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 4.1 Cc1cc(C)n(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
CHEMBL3319229 112943 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 4.1 Cc1cc(C)n(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
56942244 124664 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL3645259 124664 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
90665846 108772 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 5 0 5 6.9 Cc1ccccc1-c1nc2cc(-c3ccc(Cl)cc3)sc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218646 108772 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 5 0 5 6.9 Cc1ccccc1-c1nc2cc(-c3ccc(Cl)cc3)sc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
11339816 75639 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205521 75639 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44409756 76399 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206820 76399 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
90666012 108794 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3cccc(Cl)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218885 108794 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3cccc(Cl)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666031 108813 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 498 7 0 8 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218904 108813 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 498 7 0 8 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44390840 123026 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL361804 123026 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
90666017 108799 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218890 108799 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666027 108809 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 502 8 0 9 3.7 COC[C@H](C)N1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218900 108809 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 502 8 0 9 3.7 COC[C@H](C)N1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
44445594 154093 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 611 11 3 7 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399447 154093 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 611 11 3 7 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90666013 108795 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1cccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218886 108795 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1cccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44445599 93737 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 581 10 3 6 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL249639 93737 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 581 10 3 6 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44446187 94171 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252255 94171 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
178024 1932 30 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1932 30 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1932 30 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
23648244 91568 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241775 91568 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
44409776 76775 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207754 76775 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178616 120825 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 120825 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
16113471 84283 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 623 10 4 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL222789 84283 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 623 10 4 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
156021766 177543 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 177543 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145959787 161723 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145953855 161953 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 161953 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
16113585 136698 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL375161 136698 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
145958774 161704 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 161704 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
156016073 177071 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4641503 177071 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
162646061 178941 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of GHSR-1A (unknown origin)Inhibition of GHSR-1A (unknown origin)
ChEMBL 729 18 11 12 -5.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CO)NC(=O)CN)C(N)=O 10.1039/d0md00210k
CHEMBL4741413 178941 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of GHSR-1A (unknown origin)Inhibition of GHSR-1A (unknown origin)
ChEMBL 729 18 11 12 -5.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CO)NC(=O)CN)C(N)=O 10.1039/d0md00210k
70692600 75506 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048813 75506 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2310886 207736 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCNC(=O)CCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
156021766 177543 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 177543 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445601 93738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 498 8 2 5 5.4 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
CHEMBL249640 93738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 498 8 2 5 5.4 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
44390901 63733 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(OC)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180755 63733 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(OC)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
145959787 161723 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
70694648 75504 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048811 75504 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
44445591 154092 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399446 154092 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113468 141256 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL386218 141256 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
16113468 141256 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL386218 141256 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
46882103 5862 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079872 5862 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
72190450 91829 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426679 91829 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
11441978 129920 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 8 2 4 4.8 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL368034 129920 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 8 2 4 4.8 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL2310894 207742 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)c1ccccc1)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1021/jm0001727
122180017 121051 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586023 121051 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44445592 93736 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL249638 93736 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113577 84498 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL223725 84498 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
16113902 137138 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375859 137138 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90666041 108823 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 8 0 9 4.6 Cc1ncccc1-c1nc2cn(-c3cccc(OC(C)C)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218914 108823 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 8 0 9 4.6 Cc1ncccc1-c1nc2cn(-c3cccc(OC(C)C)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
16113902 137138 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL375859 137138 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
15945877 146394 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392593 146394 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
11337482 76272 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL206399 76272 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
44409775 75657 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205605 75657 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122182190 121482 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121482 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44445620 154128 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399651 154128 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
11676995 65816 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184258 65816 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
16203930 83904 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1cc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
CHEMBL221674 83904 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1cc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
11537683 75161 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL204352 75161 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
122180020 121054 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586026 121054 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44338247 7830 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 549 11 1 6 4.8 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL109035 7830 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 549 11 1 6 4.8 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCC1 10.1016/j.bmcl.2003.11.012
44445622 154129 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 11 4 7 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccc2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399653 154129 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 11 4 7 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccc2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
59446139 81175 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163449 81175 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436812 91318 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 11 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241033 91318 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 11 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11731384 162158 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
CHEMBL417092 162158 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
44390888 64070 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 435 7 2 4 2.7 CCN(CC)CCN1C(=O)C(O)(c2ccccc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL181312 64070 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 435 7 2 4 2.7 CCN(CC)CCN1C(=O)C(O)(c2ccccc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
60195112 81180 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 875 21 10 8 2.6 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163466 81180 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 875 21 10 8 2.6 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2370788 208166 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020985q
16113904 136499 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374655 136499 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90665852 108778 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218652 108778 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666032 108814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 512 7 0 8 4.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218905 108814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 512 7 0 8 4.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113904 136499 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374655 136499 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL500703 212339 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
10415364 126233 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat Growth hormone secretagogue receptorInhibitory concentration against rat Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126233 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat Growth hormone secretagogue receptorInhibitory concentration against rat Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
53390181 91825 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426675 91825 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
145957075 161717 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 161717 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145956026 162100 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162100 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145956061 162131 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162131 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
145951150 162214 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162214 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
11328064 159753 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 6 2 4 4.9 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OC(C)(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL411055 159753 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 6 2 4 4.9 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OC(C)(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
44445607 166166 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.4 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL428314 166166 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.4 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113581 84699 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1cccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL224921 84699 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1cccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
90666022 108804 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 7 0 9 4.2 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218895 108804 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 7 0 9 4.2 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666028 108810 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 511 7 0 10 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5cnco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218901 108810 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 511 7 0 10 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5cnco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
70682036 75510 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048817 75510 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
16113796 84244 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL222518 84244 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
57422697 112949 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319276 112949 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
44582528 192803 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm8014519
91935097 192803 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm8014519
CHEMBL525994 192803 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm8014519
CHEMBL499371 212314 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC(N)=O)C(N)=O 10.1074/jbc.m609796200
59446101 81190 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163477 81190 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446101 81190 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163477 81190 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44389262 121505 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
CHEMBL359506 121505 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
16113796 84244 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL222518 84244 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11576960 66764 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187427 66764 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
11124146 98683 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL281173 98683 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
122178600 120809 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 120809 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
44409679 75142 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204322 75142 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
9745 2410 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
9804938 2410 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
CHEMBL278623 2410 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
DB13074 2410 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
16113579 84499 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 10 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL223726 84499 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 10 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL3578015 210009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
145954311 161924 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 161924 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL3578015 210009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
11373823 78079 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)c3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211188 78079 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)c3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
145954311 161924 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 161924 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44301389 11155 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179118 11155 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL61292 11155 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
46882236 5680 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 8 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078608 5680 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 8 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
16114514 78733 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
CHEMBL2113322 78733 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
11523411 75189 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
CHEMBL204511 75189 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
57422730 112926 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 508 9 2 7 4.4 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319212 112926 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 508 9 2 7 4.4 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
46882763 5537 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK0677 from human GHS-R1aDisplacement of [35S]MK0677 from human GHS-R1a
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077617 5537 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK0677 from human GHS-R1aDisplacement of [35S]MK0677 from human GHS-R1a
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44576247 212441 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 212441 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
145951150 162214 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162214 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL433540 211884 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020424z
1744826 62654 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1021/jm0491750
CHEMBL178668 62654 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1021/jm0491750
1744826 62654 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178668 62654 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
122178603 120812 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 120812 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
16114009 136657 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 556 10 3 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374921 136657 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 556 10 3 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
23648246 161227 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL414132 161227 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
11655578 169455 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL444277 169455 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
1744826 62654 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178668 62654 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
156021336 177583 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4649089 177583 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
44446190 94107 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL251855 94107 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44389167 123327 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL362612 123327 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338240 108639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2cc(-c3ccccc3-c3nn[nH]n3)cs2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL321403 108639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2cc(-c3ccccc3-c3nn[nH]n3)cs2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
11539587 66727 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187271 66727 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
11503585 64858 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182542 64858 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
23656300 148222 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 592 12 3 7 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)c(OC)c1 10.1021/jm0704550
CHEMBL394054 148222 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 592 12 3 7 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)c(OC)c1 10.1021/jm0704550
59446107 81193 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163480 81193 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446107 81193 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163480 81193 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436807 147767 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 547 11 3 7 4.6 COc1ccc(Cn2c(CCC3C=Nc4ccccc43)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL393692 147767 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 547 11 3 7 4.6 COc1ccc(Cn2c(CCC3C=Nc4ccccc43)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
46882237 5688 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 9 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078677 5688 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 9 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44395002 65840 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184368 65840 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
44445627 154389 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 543 10 2 7 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401084 154389 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 543 10 2 7 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113906 136686 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL375102 136686 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
70692601 75507 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048814 75507 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
145957075 161717 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 161717 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145956026 162100 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162100 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145956061 162131 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162131 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
46882271 5717 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 8 4 4 5.0 CCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078899 5717 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 8 4 4 5.0 CCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
156018364 177329 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177329 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445624 154355 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 631 11 4 7 5.8 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)[C@H]2CCCC[C@H]2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400879 154355 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 631 11 4 7 5.8 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)[C@H]2CCCC[C@H]2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16203238 136572 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
CHEMBL374757 136572 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
16113694 136656 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 609 11 4 5 6.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374920 136656 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 609 11 4 5 6.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
16114181 141396 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 10 3 5 5.0 Cc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL387109 141396 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 10 3 5 5.0 Cc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44446137 154866 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403682 154866 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
122180017 121051 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586023 121051 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44379072 12674 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188124 12674 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL535353 12674 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
16113905 84259 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL222622 84259 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11626181 123849 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363896 123849 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
42624369 188266 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582535 188266 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935102 188266 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL506930 188266 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
16113691 136183 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL374073 136183 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
90666023 108805 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218896 108805 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113691 136183 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
CHEMBL374073 136183 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
57422696 112966 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319403 112966 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
156012849 176714 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 176714 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44390860 63298 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180096 63298 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
73347725 91824 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 476 6 0 5 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4ncccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426674 91824 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 476 6 0 5 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4ncccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2013.07.044
156012849 176714 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 176714 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015928 176997 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 176997 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156018364 177329 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177329 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145949595 162162 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162162 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
1100 1572 41 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
6918297 1572 41 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
CHEMBL108335 1572 41 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
11539588 66564 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186540 66564 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
122180015 121049 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586021 121049 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122178615 120777 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 120777 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
16113798 83902 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 598 11 5 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL221662 83902 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 598 11 5 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
16113797 137596 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 637 11 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL376735 137596 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 637 11 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
16113903 167802 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1cc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
CHEMBL434573 167802 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1cc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
44338241 6448 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)s2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL108287 6448 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)s2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
44410012 137858 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377305 137858 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113122 147624 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 538 12 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
CHEMBL393565 147624 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 538 12 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
11556937 81196 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163484 81196 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11556937 81196 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163484 81196 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
9956908 12970 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190326 12970 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540604 12970 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
11329138 64114 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
CHEMBL181350 64114 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
90665848 108774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 507 7 0 6 6.1 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218648 108774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 507 7 0 6 6.1 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
23648245 91569 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241776 91569 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
145949595 162162 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162162 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
11846625 77516 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209394 77516 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
44409683 75891 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205848 75891 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46882305 5736 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 7 4 4 5.7 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccc(C(C)(C)C)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079091 5736 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 7 4 4 5.7 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccc(C(C)(C)C)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
11124146 98683 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL281173 98683 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
56942855 124666 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 601 10 2 6 7.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccc3ccccc3c2)NC(=O)OC(C)(C)C)cc1 nan
CHEMBL3645261 124666 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 601 10 2 6 7.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccc3ccccc3c2)NC(=O)OC(C)(C)C)cc1 nan
11016748 97885 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275141 97885 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44445602 93739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 537 8 3 5 5.9 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
CHEMBL249659 93739 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 537 8 3 5 5.9 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
11256439 75014 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
CHEMBL203843 75014 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
44390881 65757 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccccc2OC)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL183916 65757 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccccc2OC)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
44338151 109248 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 6 5.3 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2F)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL323026 109248 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 6 5.3 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2F)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
46882238 5691 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccccc1NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078699 5691 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccccc1NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
59446133 174452 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4567432 174452 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195284 81184 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163471 81184 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44394930 65985 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185028 65985 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
11016748 97885 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275141 97885 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
59446115 173728 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4550305 173728 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195379 81188 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163475 81188 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
46882155 5617 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 8 4 4 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078114 5617 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 8 4 4 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
11145720 66988 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 11 6 4 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC 10.1021/jm020985q
CHEMBL18853 66988 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 11 6 4 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC 10.1021/jm020985q
11846628 77344 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 2 6 4.2 CN(C(=O)C1CCCC1)c1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL208930 77344 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 2 6 4.2 CN(C(=O)C1CCCC1)c1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
156015928 176997 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 176997 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16114012 167824 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 510 9 3 5 4.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL434738 167824 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 510 9 3 5 4.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
122180018 121052 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586024 121052 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
16113582 136103 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 7 4 5 3.5 Cn1c(Cc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL373995 136103 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 7 4 5 3.5 Cn1c(Cc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
46882807 5672 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 10 4 4 3.6 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078533 5672 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 10 4 4 3.6 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
16114184 149946 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](O)CN2)cc1 10.1021/jm0704550
CHEMBL395441 149946 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](O)CN2)cc1 10.1021/jm0704550
44446188 154840 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403542 154840 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
44436817 166205 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 600 13 4 6 5.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](N)Cc3ccccc3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL428383 166205 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 600 13 4 6 5.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](N)Cc3ccccc3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44445618 161337 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 570 12 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)CCc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL415134 161337 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 570 12 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)CCc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44436887 90514 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239464 90514 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
10907396 98680 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
CHEMBL281147 98680 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
11649239 65993 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185057 65993 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
1100 1572 41 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
6918297 1572 41 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
CHEMBL108335 1572 41 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
16113580 137340 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
CHEMBL376258 137340 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
16113580 137340 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376258 137340 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44436883 145608 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
CHEMBL391980 145608 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
44436889 152511 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397594 152511 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11452801 138755 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL379191 138755 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44445625 154269 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 612 11 3 8 5.4 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400381 154269 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 612 11 3 8 5.4 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
122180019 121053 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586025 121053 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
145957443 161528 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4160928 161528 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
10864048 97923 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275373 97923 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44389187 63676 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3cccc(Cl)c3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL180722 63676 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3cccc(Cl)c3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409871 75031 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203948 75031 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145959007 161695 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 161695 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145956659 161494 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 161494 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145959787 161723 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16113248 78739 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113328 78739 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
11282247 165362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL425048 165362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11282247 165362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL425048 165362 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409802 76376 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206687 76376 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
156019457 177358 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177358 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
216208 9620 27 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9620 27 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
90666037 108819 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 484 6 0 8 3.8 Cc1ncccc1-c1nc2cn(-c3ccccc3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218910 108819 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 484 6 0 8 3.8 Cc1ncccc1-c1nc2cn(-c3ccccc3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
23648236 78727 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
CHEMBL2113317 78727 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
44383343 119823 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21 10.1021/jm0309452
CHEMBL353007 119823 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21 10.1021/jm0309452
156014693 176608 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4635089 176608 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
44389151 62161 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL178138 62161 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
44409979 140016 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381159 140016 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44395020 123501 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL363021 123501 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
16114530 84302 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 539 13 4 5 5.7 CCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222912 84302 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 539 13 4 5 5.7 CCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
59446130 81192 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163479 81192 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446130 81192 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163479 81192 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409761 75498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204880 75498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145956659 161494 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 161494 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145957443 161528 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4160928 161528 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145959007 161695 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 161695 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145959787 161723 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 161723 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11328920 143498 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 471 8 2 4 5.4 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3cccc(Cl)c3C2)cc1 10.1021/jm0491750
CHEMBL390308 143498 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 471 8 2 4 5.4 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3cccc(Cl)c3C2)cc1 10.1021/jm0491750
122178606 120815 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 120815 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
122178609 120819 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 120819 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
178024 1932 30 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1932 30 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1932 30 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
44409821 75669 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205711 75669 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46882307 5738 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 530 8 4 4 6.0 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NC(C)(C)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079108 5738 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 530 8 4 4 6.0 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NC(C)(C)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
122182044 121472 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593633 121472 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
5866 3554 3 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
9804743 3554 3 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
CHEMBL360227 3554 3 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
CHEMBL500468 212334 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm501702q
CHEMBL500468 212334 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm501702q
11683469 76338 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
CHEMBL206486 76338 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
11454617 140775 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
CHEMBL383411 140775 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
90666029 108811 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 510 7 0 9 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5ccco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218902 108811 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 510 7 0 9 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5ccco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44409672 139944 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL380971 139944 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11154823 75661 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205660 75661 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
11190594 75617 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205445 75617 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11583811 75619 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205450 75619 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
25260900 112965 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 593 10 2 9 4.3 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(N4CCOCC4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319402 112965 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 593 10 2 9 4.3 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(N4CCOCC4)ccc3Cl)sc2c1 10.1021/jm500610n
10918326 98502 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
CHEMBL279822 98502 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
44378981 13842 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1196773 13842 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL558181 13842 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
90666033 108815 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 526 7 0 8 5.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218906 108815 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 526 7 0 8 5.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113472 168429 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL439251 168429 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
66813470 76464 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ghrelin from GHS receptorDisplacement of [125I]ghrelin from GHS receptor
ChEMBL 459 6 2 6 3.3 O=C(N[C@@H]1COc2cccc(-c3ccc(CO)nc3)c2C1)c1ccc(OCC(F)(F)F)nc1 10.1016/j.bmcl.2012.06.105
CHEMBL2069411 76464 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ghrelin from GHS receptorDisplacement of [125I]ghrelin from GHS receptor
ChEMBL 459 6 2 6 3.3 O=C(N[C@@H]1COc2cccc(-c3ccc(CO)nc3)c2C1)c1ccc(OCC(F)(F)F)nc1 10.1016/j.bmcl.2012.06.105
122180022 121056 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586028 121056 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
70694649 75516 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048823 75516 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
10100708 11914 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183387 11914 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL294408 11914 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
11577349 64885 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182655 64885 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
16114098 141067 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL385131 141067 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11327400 75007 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL203782 75007 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44409455 75600 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
CHEMBL205286 75600 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
156019457 177358 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177358 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
46882306 5737 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 502 8 4 4 5.2 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079107 5737 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 502 8 4 4 5.2 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
11731384 162158 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
CHEMBL417092 162158 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
118709470 112947 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 395 3 2 5 4.6 COc1ccc2nc(NC(=O)NC(=O)c3c(Cl)cccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319274 112947 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 395 3 2 5 4.6 COc1ccc2nc(NC(=O)NC(=O)c3c(Cl)cccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL507636 212652 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
156021885 177631 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4649741 177631 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
70688404 75499 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048807 75499 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
11114279 97784 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
CHEMBL274460 97784 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
70688404 75499 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2048807 75499 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2013.07.044
16113693 137476 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376471 137476 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
216208 9620 27 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9620 27 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
11827047 98750 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
CHEMBL281578 98750 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
9745 2410 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
9804938 2410 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
CHEMBL278623 2410 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
DB13074 2410 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
16113124 120808 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581032 120808 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
44445605 154430 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401260 154430 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113578 136655 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 542 9 3 5 5.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374919 136655 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 542 9 3 5 5.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
16113584 137056 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 441 7 5 4 3.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)[nH]1 10.1021/jm070024h
CHEMBL375568 137056 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 441 7 5 4 3.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)[nH]1 10.1021/jm070024h
44389168 64527 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL182154 64527 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
11314908 141268 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 377 7 3 6 3.4 CCC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL386290 141268 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 377 7 3 6 3.4 CCC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
11846627 79299 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 363 6 3 6 3.0 CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL211581 79299 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 363 6 3 6 3.0 CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
10929048 68450 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL19220 68450 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
90666020 108802 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 500 7 0 9 3.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218893 108802 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 500 7 0 9 3.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16114403 146642 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392805 146642 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)cc1 10.1021/jm0704550
57422673 112954 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 474 4 2 7 4.1 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319282 112954 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 474 4 2 7 4.1 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
70684154 75501 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048809 75501 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
122180020 121054 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586026 121054 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
16113710 78736 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113325 78736 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
122178611 120821 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 120821 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
122178614 120824 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 120824 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
16114531 84238 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 553 14 4 5 6.1 CCCCCCn1c(CCCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222498 84238 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 553 14 4 5 6.1 CCCCCCn1c(CCCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
145974293 162462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 162462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
46882197 5650 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 10 4 4 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078403 5650 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 10 4 4 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
44409980 75812 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205790 75812 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145952740 161939 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 161939 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
44409868 76374 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206673 76374 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
156017532 177324 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177324 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11605822 123856 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363930 123856 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
162651761 179619 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 798 19 7 8 3.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
CHEMBL4749698 179619 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 798 19 7 8 3.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
70686292 75512 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048819 75512 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
10186158 97977 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL275660 97977 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
122178602 120811 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 120811 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL500468 212334 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm8014519
CHEMBL3586019 210044 4 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
122180025 121059 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
CHEMBL3586031 121059 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
156017532 177324 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177324 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145952740 161939 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 161939 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
145974293 162462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 162462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44436881 91142 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 540 10 4 6 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1cccs1)C1CCNCC1 10.1021/jm0704550
CHEMBL240746 91142 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 540 10 4 6 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1cccs1)C1CCNCC1 10.1021/jm0704550
122182189 121481 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121481 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
122180016 121050 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586022 121050 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
46882199 5669 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 438 7 4 4 4.4 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078498 5669 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 438 7 4 4 4.4 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44301462 11142 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179075 11142 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL58758 11142 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
90666042 108824 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 550 8 0 9 4.4 Cc1ncccc1-c1nc2cn(-c3cccc(OC(F)F)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218915 108824 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 550 8 0 9 4.4 Cc1ncccc1-c1nc2cn(-c3cccc(OC(F)F)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
25262771 112952 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 3 7 3.7 CC(C)NCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319280 112952 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 3 7 3.7 CC(C)NCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
42624370 188240 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582537 188240 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935104 188240 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL506624 188240 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44445617 154126 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399649 154126 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
11163070 65222 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 322 5 1 2 4.3 CCN(CC)c1ccc(NC(=O)C2CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL183123 65222 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 322 5 1 2 4.3 CCN(CC)c1ccc(NC(=O)C2CCc3ccccc3C2)cc1 10.1021/jm0491750
156012428 176726 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4636832 176726 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
46882766 5581 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077839 5581 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
44436813 146762 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 11 4 5 4.5 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL392902 146762 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 11 4 5 4.5 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44410013 76685 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207268 76685 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44235473 81191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163478 81191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
44235473 81191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163478 81191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409839 75890 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205847 75890 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16114099 136687 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375103 136687 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113372 78729 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113319 78729 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2)cc1 10.1021/jm0704550
46882273 5726 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 10 4 4 5.8 CCCCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078982 5726 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 10 4 4 5.8 CCCCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
122182044 121472 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593633 121472 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
121879 2195 19 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 2195 19 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 2195 19 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL2370788 208166 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020985q
145950261 162167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44394974 66662 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186974 66662 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
44445615 161308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL414929 161308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113370 78734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL2113323 78734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
145953016 162025 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162025 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
156012445 176751 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 176751 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10186158 97977 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL275660 97977 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
11617435 75629 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL205486 75629 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
70696689 75514 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048821 75514 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
70694647 75500 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 380 6 0 4 3.2 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048808 75500 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 380 6 0 4 3.2 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2)C3)cc1 10.1016/j.bmcl.2012.05.024
56942242 124662 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 nan
CHEMBL3645257 124662 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 nan
122178605 120814 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 120814 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
44445611 154125 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399648 154125 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
122182189 121481 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121481 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
56942385 124665 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL3645260 124665 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL501261 212354 19 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
56942099 124661 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645256 124661 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
56942243 124663 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 nan
CHEMBL3645258 124663 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 nan
122178608 120818 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 120818 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
44409673 76382 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL206741 76382 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL105462 206716 34 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11690097 76304 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL206446 76304 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
57422695 112964 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 574 10 2 9 4.6 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccn4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319401 112964 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 574 10 2 9 4.6 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccn4)ccc3Cl)sc2c1 10.1021/jm500610n
25124566 1836 6 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
5870 1836 6 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
CHEMBL3358452 1836 6 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
156013219 176905 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 176905 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145957574 161739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 161739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
46882805 5732 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 474 13 4 4 5.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079046 5732 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 474 13 4 4 5.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC)cc2)cc1 10.1016/j.bmcl.2009.08.076
53390538 91831 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426681 91831 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
178024 1932 30 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
5867 1932 30 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
CHEMBL13817 1932 30 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
44445629 161339 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 559 10 2 8 4.9 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL415136 161339 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 559 10 2 8 4.9 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16204239 135748 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL373393 135748 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
11508639 76167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL206091 76167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
216208 9620 27 None - 1 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00584-3
CHEMBL113313 9620 27 None - 1 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00584-3
11846630 138393 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 426 7 3 7 3.7 Nc1nc(N)c(-c2ccc(NC(=O)c3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378438 138393 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 426 7 3 7 3.7 Nc1nc(N)c(-c2ccc(NC(=O)c3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
156012445 176751 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 176751 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145953016 162025 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162025 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145949755 162372 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162372 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
16204241 83993 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 11 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL221996 83993 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 11 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1CCc1ccccc1 10.1021/jm070024h
11221946 140302 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL381942 140302 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
11221946 140302 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
CHEMBL381942 140302 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
46882104 5863 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079873 5863 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
145956415 161502 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 161502 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145950261 162167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162167 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11654867 75833 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205833 75833 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
10415364 126233 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126233 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
178024 1932 30 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
5867 1932 30 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL13817 1932 30 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
16114404 154346 18 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL400814 154346 18 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1016/j.bmcl.2014.11.031
90666014 108796 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3cccc(C#N)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218887 108796 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3cccc(C#N)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
44436885 145884 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 634 12 6 8 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)c(OC)c1 10.1021/jm0704550
CHEMBL392191 145884 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 634 12 6 8 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)c(OC)c1 10.1021/jm0704550
44436829 151934 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397109 151934 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
16114404 154346 18 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL400814 154346 18 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
122182047 121475 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121475 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
70684155 75517 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048824 75517 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2163483 207570 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163483 207570 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409872 74701 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 7 2 8 3.1 CCc1nc(N)nc(N2CCOCC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203581 74701 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 7 2 8 3.1 CCc1nc(N)nc(N2CCOCC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44445596 154094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 558 10 2 7 5.5 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399448 154094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 558 10 2 7 5.5 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113692 136699 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL375162 136699 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
118709504 112967 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 572 5 2 9 4.3 Cc1ccnn1-c1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319404 112967 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 572 5 2 9 4.3 Cc1ccnn1-c1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
10907396 98680 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
CHEMBL281147 98680 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
11677781 124525 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL364430 124525 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
44445606 154463 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 12 3 7 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL401467 154463 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 12 3 7 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
44379034 12800 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1189120 12800 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL538068 12800 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
44378986 12969 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190325 12969 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540603 12969 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
11697618 62255 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178289 62255 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145956415 161502 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 161502 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44436886 161394 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL415674 161394 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
145949755 162372 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162372 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
23648242 78731 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.7 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113320 78731 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.7 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
11606121 64230 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
CHEMBL181584 64230 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
122180023 121057 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
CHEMBL3586029 121057 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
44379301 12934 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190091 12934 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540093 12934 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
44338300 167269 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 525 10 1 6 4.0 CN(C)CCCN1C(=O)[C@H](Cc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL430882 167269 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 525 10 1 6 4.0 CN(C)CCCN1C(=O)[C@H](Cc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44338239 167324 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 511 9 1 6 4.2 CN(C)CCCN1C(=O)[C@H](c2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL431245 167324 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 511 9 1 6 4.2 CN(C)CCCN1C(=O)[C@H](c2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44409762 75518 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204884 75518 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180018 121052 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586024 121052 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122182189 121481 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121481 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
10032659 11931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183505 11931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL301259 11931 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
60195019 81178 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163464 81178 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
156009875 176539 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 176539 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11430583 79792 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL213704 79792 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11517629 167764 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL434330 167764 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
44409975 75423 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204835 75423 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
53391301 91828 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426678 91828 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
90666019 108801 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 464 7 0 8 3.8 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(C4CCCCC4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218892 108801 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 464 7 0 8 3.8 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(C4CCCCC4)nc3c2=O)C1 10.1039/C2MD20340E
11669486 64268 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL181736 64268 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
59446141 81194 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163481 81194 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446141 81194 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163481 81194 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436917 90204 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 4 5 5.3 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239007 90204 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 4 5 5.3 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
60165265 115685 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 453 5 1 2 6.0 CC(NC(=O)N(Cc1ccccc1Cl)C1CCN(C)CC1)c1cccc(Cl)c1Cl 10.1021/jm5003183
CHEMBL3358453 115685 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 453 5 1 2 6.0 CC(NC(=O)N(Cc1ccccc1Cl)C1CCN(C)CC1)c1cccc(Cl)c1Cl 10.1021/jm5003183
16113002 147769 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 577 12 4 7 4.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
CHEMBL393693 147769 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 577 12 4 7 4.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
44409678 140673 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382853 140673 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178604 120813 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 120813 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
10929048 68450 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL19220 68450 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
60195018 81177 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 9 7 3.2 CCC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NN(CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163463 81177 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 9 7 3.2 CCC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NN(CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44394913 126639 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365721 126639 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
11649248 66322 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185399 66322 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
44394833 126291 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365460 126291 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
11827047 98750 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
CHEMBL281578 98750 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
42624359 192788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582536 192788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935103 192788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL525751 192788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
156009875 176539 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 176539 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021942 177639 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 177639 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
122180021 121055 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586027 121055 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
11134880 98959 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL282891 98959 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
11846629 138277 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 419 7 3 7 3.1 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCO3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378118 138277 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 419 7 3 7 3.1 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCO3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11114279 97784 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
CHEMBL274460 97784 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
145952396 162441 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162441 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
122178607 120817 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 120817 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
156013219 176905 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 176905 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145957574 161739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 161739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
11846463 138699 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL378909 138699 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
9890863 131457 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)C(O)(c2ccccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL369533 131457 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)C(O)(c2ccccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
44409864 75133 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204266 75133 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180027 121061 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586033 121061 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
11430392 76356 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
CHEMBL206588 76356 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
57785737 112930 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 549 7 2 8 3.7 CN1CCCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319216 112930 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 549 7 2 8 3.7 CN1CCCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44390871 64496 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2c(Cl)cccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL182035 64496 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2c(Cl)cccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
70682037 75513 14 None 43 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048820 75513 14 None 43 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
156021297 177505 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 177505 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
90666040 108822 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 9 0 9 4.6 CCCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218913 108822 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 9 0 9 4.6 CCCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666026 108808 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218899 108808 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
16204021 84269 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL222710 84269 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
122180014 121048 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586020 121048 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
90666016 108798 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 481 5 0 9 2.9 Cc1ncccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C2COC2)C1 10.1039/C2MD20340E
CHEMBL3218889 108798 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 481 5 0 9 2.9 Cc1ncccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C2COC2)C1 10.1039/C2MD20340E
44389186 64269 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL181739 64269 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338266 109831 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 523 11 1 6 4.3 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2003.11.012
CHEMBL323974 109831 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 523 11 1 6 4.3 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2003.11.012
70692602 75508 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048815 75508 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
11455251 160755 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL412362 160755 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
156021942 177639 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 177639 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16204037 136696 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccccc1Cn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL375150 136696 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccccc1Cn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
11582836 62569 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178463 62569 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389131 63117 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 485 6 1 4 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.11.075
CHEMBL179812 63117 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 485 6 1 4 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.11.075
122180025 121059 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
CHEMBL3586031 121059 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
122178612 120822 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 120822 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
16203237 96490 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
CHEMBL266199 96490 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
44582531 188126 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm8014519
91935100 188126 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm8014519
CHEMBL504776 188126 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm8014519
59446148 174467 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CC1CCCCC1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4567800 174467 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CC1CCCCC1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
46882152 5763 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCCN)c2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079302 5763 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCCN)c2)cc1 10.1016/j.bmcl.2009.08.076
11655355 74057 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL202642 74057 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145952396 162441 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162441 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
46882764 5540 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 375 9 3 3 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077716 5540 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 375 9 3 3 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2009.08.076
16114290 136671 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374992 136671 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90666015 108797 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 483 7 0 9 3.2 COCCN1CCCC(Cn2c(-c3cccnc3C)nc3cn(-c4ccc(C#N)cc4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218888 108797 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 483 7 0 9 3.2 COCCN1CCCC(Cn2c(-c3cccnc3C)nc3cn(-c4ccc(C#N)cc4)nc3c2=O)C1 10.1039/C2MD20340E
44436831 151452 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 12 4 7 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL396681 151452 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 12 4 7 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
25262608 112951 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 6 2 7 3.8 O=C(NC(=O)c1ccccc1Cl)Nc1nc2ccc(S(=O)(=O)CCN3CCCC3)cc2s1 10.1021/jm500610n
CHEMBL3319279 112951 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 6 2 7 3.8 O=C(NC(=O)c1ccccc1Cl)Nc1nc2ccc(S(=O)(=O)CCN3CCCC3)cc2s1 10.1021/jm500610n
10918326 98502 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
CHEMBL279822 98502 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
16203918 84349 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 570 9 3 5 5.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL223239 84349 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 570 9 3 5 5.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(Br)cc1 10.1021/jm070024h
70696687 75505 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048812 75505 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
46882105 6259 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1082044 6259 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
44446189 154823 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403426 154823 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44446157 94202 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 594 13 3 8 4.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](CC(=O)OCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252501 94202 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 594 13 3 8 4.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](CC(=O)OCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
44446148 154867 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL403683 154867 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
44410008 140707 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383058 140707 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
59446143 81174 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
CHEMBL2163448 81174 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
59446143 81174 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163448 81174 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
44338221 7951 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 7 4.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=S)N1CCCN1CCOCC1 10.1016/j.bmcl.2003.11.012
CHEMBL109094 7951 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 7 4.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=S)N1CCCN1CCOCC1 10.1016/j.bmcl.2003.11.012
60195113 81181 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 787 17 9 7 2.5 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm300557t
CHEMBL2163467 81181 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 787 17 9 7 2.5 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm300557t
46882804 5731 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079045 5731 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
10864048 97923 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275373 97923 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
156016110 177114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4642043 177114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156017268 177066 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177066 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
59446118 174118 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4559602 174118 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195285 81186 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163473 81186 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436868 145538 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 9 4 5 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL391922 145538 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 9 4 5 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1c1ccccc1)C1CCNCC1 10.1021/jm0704550
44394947 168646 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL440939 168646 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
122180022 121056 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586028 121056 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
11751384 140962 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL384524 140962 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122180026 121060 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 121060 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
122182043 121471 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 121471 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
16204226 84361 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 486 12 3 5 5.1 CCCCCCn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223323 84361 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 486 12 3 5 5.1 CCCCCCn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
118709472 112950 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2sc(NC(=O)NC(=O)c3ccccc3Cl)nc2c1 10.1021/jm500610n
CHEMBL3319277 112950 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2sc(NC(=O)NC(=O)c3ccccc3Cl)nc2c1 10.1021/jm500610n
46882196 5649 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 9 4 4 3.7 CCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078402 5649 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 9 4 4 3.7 CCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
44379303 12715 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188529 12715 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL536706 12715 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL2310893 207741 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
44445614 168732 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL441567 168732 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44445598 93927 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 9 3 5 6.5 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL250807 93927 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 9 3 5 6.5 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
145949381 162153 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162153 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
44436832 151454 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 548 11 4 5 4.9 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL396682 151454 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 548 11 4 5 4.9 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44445626 96606 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 573 11 2 8 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL267197 96606 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 573 11 2 8 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90666025 108807 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218898 108807 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
156012122 176797 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 176797 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156012122 176797 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 176797 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021297 177505 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 177505 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
90666024 108806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218897 108806 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
57422776 112932 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 559 7 2 8 3.3 C#Cc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319218 112932 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 559 7 2 8 3.3 C#Cc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
162657463 180448 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 783 20 7 7 4.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
CHEMBL4759415 180448 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 783 20 7 7 4.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
44409990 76149 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205995 76149 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180024 121058 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586030 121058 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
44409758 75606 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205374 75606 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122182190 121482 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121482 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44409684 140341 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382033 140341 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113003 94296 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm701292s
CHEMBL253126 94296 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm701292s
16113003 94296 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm0704550
CHEMBL253126 94296 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm0704550
122182047 121475 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121475 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
90666030 108812 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 486 7 0 8 4.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218903 108812 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 486 7 0 8 4.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
11605333 76357 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
CHEMBL206589 76357 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
122182046 121474 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 121474 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
11281346 75650 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205568 75650 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145949381 162153 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162153 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
16204145 136016 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 492 9 3 5 4.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL373772 136016 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 492 9 3 5 4.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccccc1 10.1021/jm070024h
90666036 108818 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 479 8 0 8 3.7 COc1cccc(-n2cc3nc(CC(C)C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218909 108818 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 479 8 0 8 3.7 COc1cccc(-n2cc3nc(CC(C)C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44338235 109161 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 546 7 3 6 4.1 O=C1[C@H](Cc2c[nH]c3ccccc23)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1C1CCNCC1 10.1016/j.bmcl.2003.11.012
CHEMBL322499 109161 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 546 7 3 6 4.1 O=C1[C@H](Cc2c[nH]c3ccccc23)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1C1CCNCC1 10.1016/j.bmcl.2003.11.012
156016392 177062 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177062 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156017268 177066 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177066 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145958317 161751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 161751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145949880 162229 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162229 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950963 162244 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162244 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156016392 177062 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177062 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445608 154464 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401468 154464 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
59446116 81172 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 777 17 9 8 0.8 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163439 81172 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 777 17 9 8 0.8 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
23631387 92821 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 409 4 0 4 5.1 Cc1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL244936 92821 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 409 4 0 4 5.1 Cc1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666038 108820 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1ccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
CHEMBL3218911 108820 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1ccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
44421230 84353 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 546 8 3 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1-c1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL223269 84353 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 546 8 3 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1-c1ccc(Cl)c(Cl)c1 10.1021/jm070024h
156018460 177293 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4644587 177293 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
145950963 162244 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162244 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11618705 166374 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL428698 166374 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
44436842 146393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392592 146393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCCN2)cc1 10.1021/jm0704550
CHEMBL509976 213794 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL450217 212203 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in COS-7 cells incubated for 3 hrsDisplacement of [35S]MK677 from human ghrelin receptor expressed in COS-7 cells incubated for 3 hrs
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300414b
CHEMBL450217 212203 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(N)=O 10.1074/jbc.m609796200
10984270 98042 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL276137 98042 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44436884 91107 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240522 91107 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL444131 212171 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None NC(=O)CNC(=O)CNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1074/jbc.m609796200
60195020 81179 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 835 21 10 8 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163465 81179 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 835 21 10 8 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
59446112 172395 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)N(CC1CCCCC1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4517723 172395 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)N(CC1CCCCC1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL422461 211528 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm0001727
16114010 135747 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 613 10 4 5 6.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL373392 135747 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 613 10 4 5 6.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
16203349 165726 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 4.9 COc1ccc(CCn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL427076 165726 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 4.9 COc1ccc(CCn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11531313 62160 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178137 62160 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389283 62601 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178494 62601 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
122180019 121053 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586025 121053 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL447282 212190 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm8014519
145958317 161751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 161751 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16114008 84408 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223532 84408 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
16112910 135841 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL373507 135841 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
16112910 135841 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL373507 135841 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
44436882 145471 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL391859 145471 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
145949880 162229 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162229 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
122180024 121058 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586030 121058 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
46882154 5769 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 390 7 4 4 2.9 CCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079323 5769 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 390 7 4 4 2.9 CCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
59446145 81173 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163444 81173 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446145 81173 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163444 81173 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
11699004 65856 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184429 65856 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
11537800 75201 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
CHEMBL204564 75201 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
16203236 165698 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 512 10 3 6 4.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccs1 10.1021/jm070024h
CHEMBL426905 165698 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 512 10 3 6 4.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccs1 10.1021/jm070024h
10207327 66721 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL18725 66721 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
44445603 154429 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL401259 154429 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL502208 212369 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1074/jbc.m609796200
16113583 161190 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 469 8 4 5 3.7 Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL413856 161190 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 469 8 4 5 3.7 Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
90665849 108775 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 508 7 0 7 5.5 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3nc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218649 108775 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 508 7 0 7 5.5 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3nc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
70696688 75511 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048818 75511 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
44436816 91359 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241242 91359 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
10984270 98042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL276137 98042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44301387 11144 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179088 11144 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL59572 11144 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
11692087 62648 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178610 62648 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
122178610 120820 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 120820 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
16113695 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm701292s
CHEMBL374643 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm701292s
16113695 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374643 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113695 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374643 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
16113695 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm0704550
CHEMBL374643 136490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm0704550
44436888 152510 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 3 6 5.0 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCOCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397593 152510 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 3 6 5.0 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCOCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11692087 62648 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178610 62648 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
44409809 74700 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203578 74700 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409989 165262 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL424860 165262 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL105462 206716 34 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
90666018 108800 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 488 8 0 9 3.3 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218891 108800 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 488 8 0 9 3.3 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
11612155 140465 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL382375 140465 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
118722878 115684 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 494 5 2 4 4.8 CN1CCN([C@@H](C(=O)NNc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2Cl)CC1 10.1021/jm5003183
CHEMBL3358451 115684 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 494 5 2 4 4.8 CN1CCN([C@@H](C(=O)NNc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2Cl)CC1 10.1021/jm5003183
16114097 78732 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113321 78732 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
122182189 121481 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121481 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
25260901 112968 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319405 112968 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
122180021 121055 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586027 121055 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
11179347 76985 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL208477 76985 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44445593 154237 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400174 154237 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16203569 141189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL385803 141189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
90666034 108816 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.7 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCOC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218907 108816 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.7 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCOC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL449590 212202 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
121879 2195 19 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 2195 19 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 2195 19 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
11568561 168976 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
CHEMBL443560 168976 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
44338246 98385 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 563 11 1 6 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL278909 98385 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 563 11 1 6 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL105462 206716 34 None - 1 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/s0960-894x(99)00584-3
44409767 156688 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 437 8 3 7 3.9 CCc1nc(N)nc(NC2CC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL407647 156688 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 437 8 3 7 3.9 CCc1nc(N)nc(NC2CC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44445612 96580 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 10 3 5 5.9 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm701292s
CHEMBL266964 96580 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 10 3 5 5.9 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm701292s
44410003 75813 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205794 75813 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16203569 141189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL385803 141189 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL18872 207304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(C)(C)N)C(N)=O 10.1021/jm300557t
46882106 5770 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCN)c2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079340 5770 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCN)c2)cc1 10.1016/j.bmcl.2009.08.076
44436876 146474 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL392663 146474 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
121879 2195 19 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 2195 19 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 2195 19 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
156010733 176496 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 176496 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145962494 161513 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 161513 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145950201 162380 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 162380 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44409832 76042 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205955 76042 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
16204237 84459 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 574 10 3 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL223638 84459 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 574 10 3 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
16204343 136654 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 635 12 4 5 7.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CC(c1ccccc1)c1ccccc1 10.1021/jm070024h
CHEMBL374918 136654 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 635 12 4 5 7.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CC(c1ccccc1)c1ccccc1 10.1021/jm070024h
122178613 120823 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 120823 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
57422749 112927 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 4 2 7 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319213 112927 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 4 2 7 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44410007 76059 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205963 76059 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
118718706 114867 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3350011 114867 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
89768546 148473 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of ghrelin receptor (unknown origin) by radioligand binding assayInhibition of ghrelin receptor (unknown origin) by radioligand binding assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 148473 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of ghrelin receptor (unknown origin) by radioligand binding assayInhibition of ghrelin receptor (unknown origin) by radioligand binding assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
16114011 137597 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL376736 137597 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
11349789 78348 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211265 78348 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
16112909 143737 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 561 10 4 6 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL390503 143737 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 561 10 4 6 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44378837 12896 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1189851 12896 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL539575 12896 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
44445597 94067 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 540 10 2 5 6.1 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL251640 94067 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 540 10 2 5 6.1 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
11176805 76966 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
CHEMBL208374 76966 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
156010733 176496 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 176496 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
46882153 5768 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 528 13 4 4 5.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079322 5768 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 528 13 4 4 5.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.08.076
145950201 162380 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 162380 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
46882239 5692 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1cccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)c1 10.1016/j.bmcl.2009.08.076
CHEMBL1078700 5692 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1cccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)c1 10.1016/j.bmcl.2009.08.076
1221269 121507 12 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359530 121507 12 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44446177 94197 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252448 94197 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
16114289 98199 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL277376 98199 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
11538533 74636 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
CHEMBL203280 74636 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
10415364 126233 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Growth hormone secretagogue receptorInhibitory concentration against mouse Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126233 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Growth hormone secretagogue receptorInhibitory concentration against mouse Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL263544 208820 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0001727
122180023 121057 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
CHEMBL3586029 121057 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
118709507 112971 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 547 4 2 8 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(cc4Cl)CCN5C)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319408 112971 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 547 4 2 8 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(cc4Cl)CCN5C)sc3c2)CC1 10.1021/jm500610n
90666011 108793 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1ccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
CHEMBL3218884 108793 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1ccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
11538533 74636 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203280 74636 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
44409998 137994 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377515 137994 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
90666021 108803 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218894 108803 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
11453509 75810 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205784 75810 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44445610 161162 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL413608 161162 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
23648249 78737 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113326 78737 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
11178309 79476 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL212415 79476 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL3578018 210012 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578018 210012 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44445613 93740 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 512 9 2 5 5.4 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1 10.1021/jm701292s
CHEMBL249662 93740 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 512 9 2 5 5.4 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1 10.1021/jm701292s
16204229 83886 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL221569 83886 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
44409867 76373 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 473 8 3 7 5.0 CCc1nc(N)nc(Nc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206672 76373 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 473 8 3 7 5.0 CCc1nc(N)nc(Nc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145962494 161513 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 161513 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44389215 62734 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178838 62734 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
11211892 79791 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL213703 79791 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
122180015 121049 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586021 121049 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
59446138 81195 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163482 81195 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446138 81195 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163482 81195 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
59446127 172457 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4518972 172457 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195286 81187 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163474 81187 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
10207327 66721 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL18725 66721 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
16112911 84291 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 619 13 4 7 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL222835 84291 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 619 13 4 7 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
5311280 81183 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 1035 25 11 10 2.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H]1Cc2cccc3c2N1C(=O)[C@@H](N)CC3)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163470 81183 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 1035 25 11 10 2.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H]1Cc2cccc3c2N1C(=O)[C@@H](N)CC3)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44389243 64237 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
CHEMBL181619 64237 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
23648232 90798 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 11 3 5 4.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL240179 90798 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 11 3 5 4.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
44445616 161309 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL414930 161309 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
118709471 112948 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 361 3 2 5 3.9 COc1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319275 112948 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 361 3 2 5 3.9 COc1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
44390889 64077 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(OC)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL181313 64077 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(OC)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
46882270 5725 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078960 5725 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
156016696 177046 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177046 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL3578016 210010 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL2163348 207569 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163348 207569 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
16113800 137274 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL375972 137274 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL3578016 210010 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
156013130 176918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 176918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156016696 177046 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177046 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145950877 162433 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162433 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44358041 160772 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
91931457 160772 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL412565 160772 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
57422810 177077 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4641579 177077 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
16113246 94226 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252643 94226 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
11846624 77548 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209443 77548 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
46882272 5718 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 480 8 4 4 5.5 CC(C)c1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078900 5718 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 480 8 4 4 5.5 CC(C)c1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
9987037 11912 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183385 11912 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL294324 11912 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
56942537 124667 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 551 12 2 6 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OCC(C)C)cc1 nan
CHEMBL3645262 124667 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 551 12 2 6 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OCC(C)C)cc1 nan
57422761 112928 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 510 10 3 8 3.3 COCCNCCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319214 112928 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 510 10 3 8 3.3 COCCNCCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
57422760 112925 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 2 7 3.6 CN(C)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319211 112925 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 2 7 3.6 CN(C)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
57422791 112940 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cccc(-n5cccn5)c4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319226 112940 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cccc(-n5cccn5)c4Cl)sc3c2)CC1 10.1021/jm500610n
44445619 154127 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 5 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399650 154127 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 5 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113469 136964 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL375408 136964 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL501253 212352 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CCCCCCCBr)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm8014519
122182045 121473 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593634 121473 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
44446175 94533 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 13 3 7 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL254741 94533 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 13 3 7 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
10994861 66920 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 514 9 6 4 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL18815 66920 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 514 9 6 4 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
10984260 167779 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 529 9 7 5 1.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(N)CCNCC1 10.1021/jm020985q
CHEMBL434391 167779 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 529 9 7 5 1.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(N)CCNCC1 10.1021/jm020985q
59446135 81189 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
CHEMBL2163476 81189 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
59446135 81189 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163476 81189 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
59446154 81176 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O nan
CHEMBL2163453 81176 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O nan
59446154 81176 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O 10.1021/jm300557t
CHEMBL2163453 81176 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O 10.1021/jm300557t
44446178 154572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL402023 154572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
753168 122710 33 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL361366 122710 33 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338253 9182 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 539 11 1 6 4.4 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL110900 9182 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 539 11 1 6 4.4 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44301512 11902 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183340 11902 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL291333 11902 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
16113799 168137 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL436849 168137 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
11166495 75184 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL204474 75184 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
25262772 112953 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 521 6 2 8 2.9 CN1CCN(CCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319281 112953 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 521 6 2 8 2.9 CN1CCN(CCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44390869 121815 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL359922 121815 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
156013130 176918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 176918 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
122180014 121048 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586020 121048 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122178601 120810 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 120810 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
16202767 84558 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 9 3 5 4.8 Cc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL223810 84558 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 9 3 5 4.8 Cc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
46882156 5618 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 7 4 4 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078115 5618 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 7 4 4 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
16113474 136097 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 8 4 5 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nncn1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL373993 136097 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 8 4 5 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nncn1CCc1c[nH]c2ccccc12 10.1021/jm070024h
59446105 172242 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4514053 172242 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11556936 81185 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163472 81185 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
60195114 81182 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 640 13 8 6 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300557t
CHEMBL2163468 81182 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 640 13 8 6 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300557t
70690449 75503 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048810 75503 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
70692603 75509 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048816 75509 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
44389192 168070 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL436275 168070 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
44394982 65792 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184093 65792 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL526723 213911 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm8014519
CHEMBL335799 209808 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0001727
CHEMBL61663 214052 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/s0960-894x(01)00324-9
44445628 161338 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 6 5.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL415135 161338 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 6 5.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
145950877 162433 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162433 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
11663710 123935 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363995 123935 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
16113371 78728 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL2113318 78728 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
16113371 78728 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113318 78728 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
11713497 122708 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL361349 122708 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
122182045 121473 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593634 121473 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
11646276 75566 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL205136 75566 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
122182046 121474 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 121474 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
44436828 91554 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241664 91554 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL410108 211042 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
11538533 74636 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203280 74636 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL500468 212334 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm020985q
11538534 74649 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203373 74649 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
122182047 121475 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121475 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
70686293 75515 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048822 75515 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
122180016 121050 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586022 121050 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44389216 123323 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
CHEMBL362595 123323 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
44389248 121641 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359714 121641 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145958774 161704 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 161704 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44445609 96579 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 579 10 3 5 6.4 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL266961 96579 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 579 10 3 5 6.4 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16114532 84258 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccccc1Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222610 84258 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccccc1Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
23648250 78738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113327 78738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
44409764 76781 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207792 76781 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44378979 12720 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188586 12720 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL536779 12720 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
11197 1046 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
154699458 1046 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL4632411 1046 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL498956 212307 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm8014519
46882198 5668 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078497 5668 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL3578017 210011 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578017 210011 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
145953855 161953 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 161953 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
90666035 108817 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 437 6 0 8 2.8 COc1cccc(-n2cc3nc(C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218908 108817 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 437 6 0 8 2.8 COc1cccc(-n2cc3nc(C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
328912 62232 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
CHEMBL178266 62232 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
178024 1932 30 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
5867 1932 30 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
CHEMBL13817 1932 30 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
57398340 70917 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2ccc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956993 70917 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2ccc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57400002 70918 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ccc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956994 70918 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ccc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57394881 70934 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 489 5 0 7 4.3 Cc1nc2ncc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957010 70934 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 489 5 0 7 4.3 Cc1nc2ncc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57393073 70925 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2cnc(Oc3ccc4ncsc4c3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957001 70925 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2cnc(Oc3ccc4ncsc4c3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56926461 68679 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923609 68679 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926462 68680 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923610 68680 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926680 68693 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923623 68693 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926682 68695 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923625 68695 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11664206 68696 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923626 68696 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926893 68706 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
CHEMBL1923637 68706 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
11526745 68711 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923642 68711 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134137202 142282 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3893048 142282 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134137257 142593 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3895776 142593 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134133352 142961 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3898794 142961 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
11527086 143506 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)c(Cl)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3903118 143506 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)c(Cl)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11512561 143824 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3905791 143824 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134133037 144022 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3907497 144022 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
134132670 144069 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3907891 144069 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134132152 144387 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3910300 144387 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
134142839 144841 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913855 144841 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134142553 144902 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3914259 144902 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134143635 145029 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3915269 145029 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
134143096 145388 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 584 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Br)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3918009 145388 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 584 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Br)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134142204 145392 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3918046 145392 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11584702 145646 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3920049 145646 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139279 145902 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922056 145902 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134138445 146832 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C/c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3929593 146832 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C/c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138218 147465 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934367 147465 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148686 147627 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3935670 147627 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134149719 148143 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 2 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C(C)(C)C)C(=O)N1C nan
CHEMBL3939872 148143 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 2 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C(C)(C)C)C(=O)N1C nan
134145791 148242 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3940705 148242 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134143746 150055 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 2 4 5 3.9 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1cccc(Cl)c1 nan
CHEMBL3955179 150055 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 2 4 5 3.9 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1cccc(Cl)c1 nan
134145221 150087 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NC[C@H](C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3955437 150087 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NC[C@H](C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134155656 150650 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959816 150650 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H](C)N(C)C1=O nan
134155282 150798 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961108 150798 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153496 151741 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3969367 151741 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153654 152222 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 632 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3973513 152222 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 632 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134157569 153490 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2cc(F)c(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3984338 153490 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2cc(F)c(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
57345600 70914 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ncc(Oc3ccc(Br)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956990 70914 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ncc(Oc3ccc(Br)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57345599 70915 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2ccc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956991 70915 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2ccc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57398341 70923 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2cnc(Oc3ccc(Cl)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956999 70923 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2cnc(Oc3ccc(Cl)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
178024 1932 30 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
5867 1932 30 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
CHEMBL13817 1932 30 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
57398342 70931 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 450 5 0 9 4.0 Cc1nc2ncc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957007 70931 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 450 5 0 9 4.0 Cc1nc2ncc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401803 70933 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 469 6 0 7 5.1 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957009 70933 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 469 6 0 7 5.1 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401799 70924 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2cnc(Oc3ccc4c(c3)OCO4)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957000 70924 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2cnc(Oc3ccc4c(c3)OCO4)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57399248 68687 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923617 68687 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
44340008 112876 0 None - 1 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 583 9 2 6 3.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(C(C)(C)C)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL331801 112876 0 None - 1 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 583 9 2 6 3.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(C(C)(C)C)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
57399248 68687 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923617 68687 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
24970113 68699 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923629 68699 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
57391293 70921 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ccc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956997 70921 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ccc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162659411 180633 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 575 13 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CC#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761419 180633 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 575 13 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CC#N)cc1 10.1021/acs.jmedchem.9b02122
44340268 110019 0 None - 1 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 609 10 2 6 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL325062 110019 0 None - 1 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 609 10 2 6 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
57401800 70927 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 446 5 0 8 3.9 Cc1nc2cnc(Oc3ccc4c(c3)ncn4C)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957003 70927 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 446 5 0 8 3.9 Cc1nc2cnc(Oc3ccc4c(c3)ncn4C)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162657606 180525 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760409 180525 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
57401801 70929 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 445 5 0 7 4.2 Cc1nc2ncc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957005 70929 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 445 5 0 7 4.2 Cc1nc2ncc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162672839 182430 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4793824 182430 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL500468 212334 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm300414b
56942242 124662 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 124662 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
56925343 68709 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923640 68709 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
57398339 70916 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2ccc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956992 70916 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2ccc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162645413 179136 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744051 179136 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
155540883 172378 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172378 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
16133832 211573 15 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
CHEMBL425281 211573 15 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
162653781 179890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753046 179890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
57401802 70930 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 437 5 0 9 3.1 Cc1nc2ncc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957006 70930 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 437 5 0 9 3.1 Cc1nc2ncc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401797 70910 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956987 70910 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57398343 70932 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 462 5 0 8 4.1 Cc1nc2ncc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957008 70932 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 462 5 0 8 4.1 Cc1nc2ncc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56926175 68656 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923504 68656 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926360 68678 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923608 68678 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926582 68686 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923616 68686 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926681 68694 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923624 68694 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926891 68704 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923635 68704 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926892 68705 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923636 68705 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926894 68707 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923638 68707 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
56925345 68712 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923643 68712 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134130631 141829 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
CHEMBL3889512 141829 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
134131442 141852 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3889678 141852 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134131183 141924 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890296 141924 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134136433 141963 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(OC)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890602 141963 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(OC)c2)NC(=O)C2(CCCC2)NC1=O nan
134137008 141999 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890889 141999 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134137012 142058 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 3 3 6 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccsc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3891381 142058 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 3 3 6 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccsc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134137398 142332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 4 4.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3893476 142332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 4 4.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134136665 142355 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 5 6 3.9 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(O)cc1 nan
CHEMBL3893697 142355 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 5 6 3.9 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(O)cc1 nan
134133488 142692 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3896536 142692 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134248 142807 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3897510 142807 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134134556 142808 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3897527 142808 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134133518 142909 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3898348 142909 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134134286 143150 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3900284 143150 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134135296 143467 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 4 5 3.0 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3902856 143467 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 4 5 3.0 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134132958 144116 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
CHEMBL3908264 144116 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
134132137 144268 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)cc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3909431 144268 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)cc2)NC(=O)C(C)N(C)C1=O nan
134132893 144318 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3909834 144318 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
24969783 144319 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc(F)cc2O1 nan
CHEMBL3909838 144319 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc(F)cc2O1 nan
130334810 144615 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C2=O)N(C)C1=O nan
CHEMBL3912211 144615 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C2=O)N(C)C1=O nan
134132394 144639 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccn2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3912375 144639 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccn2)NC(=O)[C@@H](C)N(C)C1=O nan
134142218 144742 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3913052 144742 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
134142433 144781 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3913335 144781 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
59778970 144830 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 6 1.8 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913763 144830 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 6 1.8 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134143366 145215 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3916659 145215 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
117812386 145313 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3917385 145313 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139489 145517 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2cc(F)cc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3919021 145517 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2cc(F)cc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134140270 145828 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3921499 145828 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134140007 145859 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3921750 145859 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139286 146009 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922810 146009 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134139113 146108 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)N(C)C1=O nan
CHEMBL3923633 146108 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)N(C)C1=O nan
134141159 146184 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3924192 146184 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
134140968 146245 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCNC(C2CC2)C(=O)N1C nan
CHEMBL3924635 146245 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCNC(C2CC2)C(=O)N1C nan
134141782 146449 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3926434 146449 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134141886 146573 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3927481 146573 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134138234 146868 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 3 5 2.4 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc3c(c2)OC(CC3)CN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3929852 146868 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 3 5 2.4 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc3c(c2)OC(CC3)CN[C@@H](C2CC2)C(=O)N1C nan
117812380 147207 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3932408 147207 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138595 147210 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
CHEMBL3932434 147210 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
134138824 147470 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934402 147470 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148504 147810 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3937200 147810 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149092 147909 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3937924 147909 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134149306 147930 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3938104 147930 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134149407 147976 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 571 4 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C#N)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3938452 147976 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 571 4 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C#N)c2)NC(=O)C2(CCCC2)NC1=O nan
134148639 147999 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 5 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCNC2)NC1=O nan
CHEMBL3938683 147999 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 5 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCNC2)NC1=O nan
134146570 148236 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3940653 148236 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145552 148475 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(CC)C1=O nan
CHEMBL3942528 148475 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(CC)C1=O nan
134145564 148546 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3943086 148546 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
72574018 148560 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NCC(C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3943159 148560 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NCC(C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134146319 148582 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CC(C)CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3943294 148582 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CC(C)CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134147809 148905 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3946007 148905 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134147441 148945 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3946348 148945 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134146888 149219 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 624 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Br)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3948268 149219 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 624 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Br)c2)NC(=O)C2(CCCC2)NC1=O nan
134147381 149241 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3948472 149241 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134147802 149547 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3950904 149547 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134145064 149605 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3951476 149605 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134144205 149729 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3952596 149729 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
134144429 149741 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3952699 149741 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134144211 149786 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2C#CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3953033 149786 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2C#CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134144606 149790 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3953053 149790 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
134155024 150468 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3958451 150468 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155239 150470 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3958460 150470 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
134155132 150548 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959108 150548 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
134155178 150835 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCNC(C2CC2)C(=O)N1C nan
CHEMBL3961456 150835 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCNC(C2CC2)C(=O)N1C nan
134150646 151102 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 5 3 6 2.6 CSCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3963865 151102 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 5 3 6 2.6 CSCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134150029 151571 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967783 151571 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134150729 151612 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 2.1 CC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3968175 151612 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 2.1 CC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154254 151755 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3969506 151755 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154486 151898 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
CHEMBL3970827 151898 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
134154392 151988 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3971540 151988 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134153247 152176 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3973085 152176 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
134153772 152354 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccs2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3974701 152354 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccs2)NC(=O)[C@@H](C)N(C)C1=O nan
52911621 152515 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 531 3 3 6 1.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(C#N)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3975975 152515 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 531 3 3 6 1.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(C#N)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134151758 152558 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(Cl)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3976294 152558 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(Cl)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134152984 152622 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3976853 152622 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
134151899 152773 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3978207 152773 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
134152339 152913 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 545 3 4 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3979468 152913 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 545 3 4 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134152133 152977 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 3 4 6 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(O)c(C(C)(C)C)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3979911 152977 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 3 4 6 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(O)c(C(C)(C)C)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134157813 153126 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 4 3 6 1.7 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3981238 153126 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 4 3 6 1.7 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134156963 153312 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3982825 153312 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O nan
57528321 153411 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 2 2 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCCC[C@H]2C(=O)N1C nan
CHEMBL3983626 153411 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 2 2 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCCC[C@H]2C(=O)N1C nan
134156579 153508 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3984464 153508 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134156405 153716 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 620 4 4 6 4.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccsc1 nan
CHEMBL3986375 153716 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 620 4 4 6 4.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccsc1 nan
134156453 153754 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccncc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3986628 153754 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccncc2)NC(=O)[C@@H](C)N(C)C1=O nan
56942098 124660 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 124660 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
162646324 179146 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744139 179146 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
162665018 181543 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 550 12 3 6 4.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(C)=O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4782214 181543 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 550 12 3 6 4.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(C)=O)cc1 10.1021/acs.jmedchem.9b02122
58438451 91839 0 None 2089 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 442 4 0 6 3.1 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426689 91839 0 None 2089 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 442 4 0 6 3.1 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
90644553 111230 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 540 5 1 7 4.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ccc(C(N)=O)nc6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287214 111230 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 540 5 1 7 4.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ccc(C(N)=O)nc6)ccc53)C4)nc2s1 10.1021/ml400473x
56926177 68658 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923506 68658 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926268 68660 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O nan
CHEMBL1923510 68660 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O nan
56926269 68661 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O nan
CHEMBL1923511 68661 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O nan
56926356 68662 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
CHEMBL1923512 68662 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
56926465 68683 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL1923613 68683 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
56926782 68700 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923631 68700 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926784 68702 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923633 68702 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926785 68703 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923634 68703 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
71452183 83102 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O nan
CHEMBL2203623 83102 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O nan
134131439 141851 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 527 4 4 6 1.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCN)C(=O)N1C nan
CHEMBL3889672 141851 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 527 4 4 6 1.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCN)C(=O)N1C nan
134137460 142091 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3891657 142091 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
134136637 142176 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 541 5 4 6 1.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCN)C(=O)N1C nan
CHEMBL3892319 142176 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 541 5 4 6 1.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCN)C(=O)N1C nan
134136946 142210 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccc(C(=O)O)cc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3892517 142210 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccc(C(=O)O)cc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134136405 142375 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 616 4 4 5 4.6 CC[C@H](C)[C@@H]1NCCOc2ccc(Cl)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3893850 142375 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 616 4 4 5 4.6 CC[C@H](C)[C@@H]1NCCOc2ccc(Cl)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134133771 142797 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 4 3 5 2.3 CCC[C@H]1NC(=O)[C@@H](C)N(C)C(=O)[C@H]([C@@H](C)CC)NCCOc2ccccc2CCCNC1=O nan
CHEMBL3897387 142797 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 4 3 5 2.3 CCC[C@H]1NC(=O)[C@@H](C)N(C)C(=O)[C@H]([C@@H](C)CC)NCCOc2ccccc2CCCNC1=O nan
134133353 142975 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)N(C)C1=O nan
CHEMBL3898864 142975 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)N(C)C1=O nan
134134505 143124 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 4 4.3 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3900035 143124 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 4 4.3 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134605 143133 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3900122 143133 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
134134099 143187 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 639 4 4 6 4.1 N#Cc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3900636 143187 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 639 4 4 6 4.1 N#Cc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134135897 143450 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 530 4 4 4 4.0 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3902804 143450 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 530 4 4 4 4.0 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134825 143535 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 476 3 3 5 1.4 C[C@@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NCCCCCOCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3903351 143535 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 476 3 3 5 1.4 C[C@@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NCCCCCOCCN[C@@H](C2CC2)C(=O)N1C nan
72989837 143571 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)NC(=O)C(CO)N(C)C1=O nan
CHEMBL3903647 143571 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)NC(=O)C(CO)N(C)C1=O nan
134135712 143594 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
CHEMBL3903845 143594 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
134136025 143788 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3905495 143788 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134134870 143847 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3905987 143847 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134135261 143940 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC)N(C)C1=O nan
CHEMBL3906788 143940 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC)N(C)C1=O nan
134134893 143966 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
CHEMBL3907031 143966 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
134132666 144020 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3907480 144020 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134132519 144104 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccsc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3908156 144104 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccsc2)NC(=O)C2(CCCC2)NC1=O nan
134132427 144156 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 622 5 4 5 5.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3908583 144156 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 622 5 4 5 5.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)C2(CCCC2)NC1=O nan
134131971 144383 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3910288 144383 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134132265 144426 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
CHEMBL3910661 144426 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
134131903 144593 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 529 4 3 7 2.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cscn2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3912034 144593 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 529 4 3 7 2.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cscn2)NC(=O)[C@@H](C)N(C)C1=O nan
134132099 144665 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccs2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3912534 144665 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccs2)NC(=O)C2(CCCC2)NC1=O nan
134142223 144798 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 480 4 4 5 1.7 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CNC1=O nan
CHEMBL3913486 144798 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 480 4 4 5 1.7 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CNC1=O nan
134142139 144857 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 5 4 6 3.6 COc1ccc(C[C@@H]2NCCOc3ccccc3/C=C\CNC(=O)[C@H](Cc3ccccc3)NC(=O)C3(CCCC3)NC2=O)cc1 nan
CHEMBL3913981 144857 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 5 4 6 3.6 COc1ccc(C[C@@H]2NCCOc3ccccc3/C=C\CNC(=O)[C@H](Cc3ccccc3)NC(=O)C3(CCCC3)NC2=O)cc1 nan
76460236 144915 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3914338 144915 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134143044 144928 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3914467 144928 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
134143657 145191 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 1.4 COC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3916501 145191 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 1.4 COC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134143398 145389 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCC(C)(C)c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3918022 145389 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCC(C)(C)c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139992 145794 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccccc1Cl nan
CHEMBL3921227 145794 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccccc1Cl nan
134140213 146075 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 513 3 4 6 0.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CN)C(=O)N1C nan
CHEMBL3923324 146075 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 513 3 4 6 0.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CN)C(=O)N1C nan
134140762 146120 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 2 5 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C1=O)C2=O nan
CHEMBL3923718 146120 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 2 5 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C1=O)C2=O nan
134141057 146150 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CCC1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3923918 146150 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CCC1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134140844 146680 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc(Cl)c1 nan
CHEMBL3928367 146680 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc(Cl)c1 nan
68186750 146842 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 CC1CCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc21 nan
CHEMBL3929656 146842 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 CC1CCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc21 nan
134138656 147009 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3930811 147009 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134138764 147091 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 3 7 2.1 COc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1OC nan
CHEMBL3931402 147091 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 3 7 2.1 COc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1OC nan
134138160 147120 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 6 1.4 CCC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3931716 147120 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 6 1.4 CCC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)N(C)C1=O nan
134137758 147429 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 500 7 4 5 3.2 CCCC[C@@H]1NC(=O)[C@H](CCCC)NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
CHEMBL3934093 147429 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 500 7 4 5 3.2 CCCC[C@@H]1NC(=O)[C@H](CCCC)NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
134137945 147441 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 3 4 5 3.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O nan
CHEMBL3934184 147441 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 3 4 5 3.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O nan
134149048 147532 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 5 6 1.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1CO nan
CHEMBL3934901 147532 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 5 6 1.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1CO nan
134149058 147590 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 586 4 4 6 3.6 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccs1 nan
CHEMBL3935422 147590 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 586 4 4 6 3.6 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccs1 nan
134149451 147621 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3935626 147621 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134148804 147774 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 6 2.9 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCSCC2)NC1=O nan
CHEMBL3936957 147774 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 6 2.9 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCSCC2)NC1=O nan
58012657 147821 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 4 3 5 3.9 CCC[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3937314 147821 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 4 3 5 3.9 CCC[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
134149772 147935 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 4 4 4 5.0 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3938132 147935 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 4 4 4 5.0 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134149793 148061 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
CHEMBL3939196 148061 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
134148754 148155 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 646 8 3 6 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C(COCc2ccccc2)N(C)C1=O nan
CHEMBL3939993 148155 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 646 8 3 6 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C(COCc2ccccc2)N(C)C1=O nan
134145258 148258 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 4 4.8 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3940860 148258 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 4 4.8 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134145652 148479 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 6 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3942543 148479 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 6 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145920 148482 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 4 5 2.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3942554 148482 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 4 5 2.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134146710 148486 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 4 7 3.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cscn1 nan
CHEMBL3942610 148486 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 4 7 3.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cscn1 nan
134145820 148490 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3942642 148490 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134146617 148571 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.0 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3943228 148571 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.0 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145420 148769 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)N(C)C1=O nan
CHEMBL3944936 148769 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)N(C)C1=O nan
134147617 148891 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3945918 148891 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134147244 148902 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 4 6 2.0 CC[C@H](C)[C@@H]1NCCOCCOCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3945984 148902 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 4 6 2.0 CC[C@H](C)[C@@H]1NCCOCCOCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134148131 149154 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 568 4 4 6 2.6 COC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3947758 149154 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 568 4 4 6 2.6 COC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134147387 149273 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 4 4 3.9 CC[C@H](C)[C@@H]1NCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3948746 149273 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 4 4 3.9 CC[C@H](C)[C@@H]1NCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134147861 149313 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 2 4 5 2.9 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3949023 149313 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 2 4 5 2.9 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C(C)(C)NC1=O nan
134147972 149394 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3949704 149394 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
134147412 149422 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3949926 149422 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
134148083 149567 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 3 4 5 3.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCCC2)NC1=O nan
CHEMBL3951110 149567 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 3 4 5 3.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCCC2)NC1=O nan
134144491 149596 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 4 4 3.5 CC[C@H](C)[C@@H]1NCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3951362 149596 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 4 4 3.5 CC[C@H](C)[C@@H]1NCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134143693 149612 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.1 CC[C@H](C)[C@@H]1NCCOCCCCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3951593 149612 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.1 CC[C@H](C)[C@@H]1NCCOCCCCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134145200 149907 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3954124 149907 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134144043 149944 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 4 5 6 2.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1c[nH]cn1 nan
CHEMBL3954394 149944 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 4 5 6 2.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1c[nH]cn1 nan
134144941 149982 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3954620 149982 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134144060 150112 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3955632 150112 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134155541 150493 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CCC(C)C1NCCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3958657 150493 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CCC(C)C1NCCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134155247 150506 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc2ccccc2c1 nan
CHEMBL3958739 150506 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc2ccccc2c1 nan
117812381 150807 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 3 3 5 3.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(C(F)(F)F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3961160 150807 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 3 3 5 3.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(C(F)(F)F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134155292 150858 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 458 4 3 5 1.3 CC[C@H](C)[C@@H]1NCCOC/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961641 150858 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 458 4 3 5 1.3 CC[C@H](C)[C@@H]1NCCOC/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154704 150866 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 2 4 5 3.1 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)C2(CCCC2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3961696 150866 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 2 4 5 3.1 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)C2(CCCC2)NC(=O)C2(CCCC2)NC1=O nan
134152627 151004 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3963078 151004 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134150950 151061 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 5 4 5 2.8 CCC[C@@H]1NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3963523 151061 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 5 4 5 2.8 CCC[C@@H]1NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC1=O nan
57528212 151279 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 2 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCC[C@H]2C(=O)N1C nan
CHEMBL3965338 151279 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 2 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCC[C@H]2C(=O)N1C nan
134150767 151282 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3965351 151282 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134150369 151312 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2cc(F)ccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)N(C)C1=O nan
CHEMBL3965516 151312 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2cc(F)ccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)N(C)C1=O nan
134150388 151381 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(NS(C)(=O)=O)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3966251 151381 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(NS(C)(=O)=O)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134150696 151535 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967506 151535 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134153608 151826 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3970180 151826 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154369 151850 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3970414 151850 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153972 151858 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 3 3 6 1.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3970491 151858 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 3 3 6 1.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134154079 151859 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970499 151859 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
134153529 151904 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 5 4 5 3.4 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970856 151904 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 5 4 5 3.4 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134154612 151967 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@H](C2=O)N(C)C1=O nan
CHEMBL3971356 151967 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@H](C2=O)N(C)C1=O nan
134153232 152035 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.5 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1Cc1ccccc1 nan
CHEMBL3971845 152035 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.5 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1Cc1ccccc1 nan
134154534 152200 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 1.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC/C=C\COCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3973254 152200 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 1.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC/C=C\COCCN[C@@H](C2CC2)C(=O)N1C nan
134154022 152281 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3973940 152281 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134151581 152662 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3977241 152662 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
57528347 152666 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
CHEMBL3977265 152666 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
134152388 152672 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 5 4 5 4.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1CCc1ccccc1 nan
CHEMBL3977294 152672 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 5 4 5 4.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1CCc1ccccc1 nan
134151706 152808 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3978455 152808 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134151524 152834 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 644 5 4 6 4.2 COc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3978661 152834 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 644 5 4 6 4.2 COc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134152209 152856 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 3 4 6 1.0 CC(O)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3978864 152856 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 3 4 6 1.0 CC(O)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134152547 152937 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 2.9 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3979606 152937 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 2.9 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11421086 153020 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 2 5 2.8 CCC[C@H]1C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN1C nan
CHEMBL3980276 153020 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 2 5 2.8 CCC[C@H]1C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN1C nan
134157913 153085 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 3 4 5 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3980873 153085 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 3 4 5 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134156625 153105 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3981072 153105 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134157438 153202 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 5 5 1.9 CC[C@H](C)[C@@H]1NCCCNCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3981843 153202 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 5 5 1.9 CC[C@H](C)[C@@H]1NCCCNCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134157625 153215 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3981960 153215 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
59834193 153606 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.5 CC1CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc2C1 nan
CHEMBL3985477 153606 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.5 CC1CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc2C1 nan
134156443 153800 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)N(C)C1=O nan
CHEMBL3986906 153800 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)N(C)C1=O nan
56926176 68657 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923505 68657 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926266 68659 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O nan
CHEMBL1923508 68659 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O nan
134133634 143090 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 549 4 4 6 2.7 CC(C)C[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3899825 143090 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 549 4 4 6 2.7 CC(C)C[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
57722117 143140 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 466 2 3 5 1.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3900193 143140 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 466 2 3 5 1.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
57722068 143389 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOCCOCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3902231 143389 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOCCOCCN[C@@H](C2CC2)C(=O)N1C nan
134135595 143420 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 4 4 5 5.1 CC(C)C[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3902597 143420 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 4 4 5 5.1 CC(C)C[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134139160 145664 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 4 3 5 3.7 CC(C)C[C@H]1C(=O)NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN1C nan
CHEMBL3920156 145664 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 4 3 5 3.7 CC(C)C[C@H]1C(=O)NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN1C nan
134140250 145701 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 562 5 4 5 3.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](CCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3920479 145701 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 562 5 4 5 3.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](CCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
57951693 145732 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
CHEMBL3920711 145732 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
134140177 145825 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC(C)C[C@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3921493 145825 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC(C)C[C@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134139639 146094 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 6 4 7 2.5 CCOC(=O)CC[C@@H]1NC(=O)C2(CCCC2)NC(=O)[C@H](CC(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
CHEMBL3923467 146094 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 6 4 7 2.5 CCOC(=O)CC[C@@H]1NC(=O)C2(CCCC2)NC(=O)[C@H](CC(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
134140216 146099 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 5 5 3.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3923508 146099 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 5 5 3.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
134141155 146183 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 6 3.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3924187 146183 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 6 3.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCOC2)NC1=O nan
134137626 146938 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 5 6 3.0 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3930400 146938 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 5 6 3.0 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C2(CCCC2)NC1=O nan
134148332 147737 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ncccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3936664 147737 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ncccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
57528213 147940 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
CHEMBL3938163 147940 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
134149424 148092 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](C(C)c2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3939431 148092 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](C(C)c2ccccc2)NC(=O)CN(C)C1=O nan
57951672 149050 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3946954 149050 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
134147008 149392 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 4 5 2.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3949653 149392 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 4 5 2.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134155726 150474 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCOCCOCCNC(C2CC2)C(=O)N1C nan
CHEMBL3958492 150474 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCOCCOCCNC(C2CC2)C(=O)N1C nan
134155844 150544 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 6 4 5 3.3 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC1=O nan
CHEMBL3959055 150544 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 6 4 5 3.3 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC1=O nan
57528307 150583 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
CHEMBL3959346 150583 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
134156186 150806 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 490 4 4 4 3.1 CC[C@H](C)[C@@H]1NCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3961157 150806 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 490 4 4 4 3.1 CC[C@H](C)[C@@H]1NCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134150525 151020 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 551 8 5 6 2.2 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O nan
CHEMBL3963236 151020 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 551 8 5 6 2.2 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O nan
134149894 151290 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3965402 151290 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(Cl)cc1 nan
134150119 151503 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 6 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](COC(C)(C)C)NC1=O nan
CHEMBL3967266 151503 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 6 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](COC(C)(C)C)NC1=O nan
134150914 151536 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)CC)N(C)C1=O nan
CHEMBL3967522 151536 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)CC)N(C)C1=O nan
57722047 152322 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 436 4 3 4 1.8 CCC[C@@H]1NCc2cccc(c2)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3974323 152322 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 436 4 3 4 1.8 CCC[C@@H]1NCc2cccc(c2)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
57951687 152327 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
CHEMBL3974356 152327 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
57528291 152371 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
CHEMBL3974776 152371 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
134152485 152630 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 604 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(C(=O)O)cc2)NC(=O)C2(CCCC2)N(C)C1=O nan
CHEMBL3976941 152630 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 604 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(C(=O)O)cc2)NC(=O)C2(CCCC2)N(C)C1=O nan
134151873 152654 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc2ccccc12 nan
CHEMBL3977166 152654 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc2ccccc12 nan
76556607 153009 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)N2CCC(C2=O)N(C)C1=O nan
CHEMBL3980176 153009 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)N2CCC(C2=O)N(C)C1=O nan
134157812 153124 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 4 5 2.1 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3981235 153124 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 4 5 2.1 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134156737 153153 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 547 4 4 6 2.8 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccncc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3981446 153153 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 547 4 4 6 2.8 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccncc2)NC(=O)C2(CCCC2)NC1=O nan
134156806 153548 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 6 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O nan
CHEMBL3984892 153548 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 6 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O nan
134157124 153660 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 2 4 5 1.9 O=C1CNCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)N1 nan
CHEMBL3985913 153660 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 2 4 5 1.9 O=C1CNCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)N1 nan
11706547 68689 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 3 3 5 2.8 CC(C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923619 68689 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 3 3 5 2.8 CC(C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
134138625 147486 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3934561 147486 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
44434011 147319 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL393321 147319 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
70692601 75507 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048814 75507 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
127046957 139164 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 139164 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
127046472 139151 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798056 139151 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
56926266 68659 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O 10.1021/jm2007062
CHEMBL1923508 68659 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O 10.1021/jm2007062
73352329 91819 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426669 91819 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
70692602 75508 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048815 75508 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
162665974 181643 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 612 13 3 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4783347 181643 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 612 13 3 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
44396381 67176 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 558 13 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL189625 67176 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 558 13 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm040103i
44396377 66594 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 13 2 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(Cc1ccc(C)o1)C(=O)NC1CCCCC1 10.1021/jm040103i
CHEMBL186647 66594 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 13 2 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(Cc1ccc(C)o1)C(=O)NC1CCCCC1 10.1021/jm040103i
44396269 67004 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 426 10 2 3 4.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC(C)(C)C 10.1021/jm040103i
CHEMBL188586 67004 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 426 10 2 3 4.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC(C)(C)C 10.1021/jm040103i
56926895 68708 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 3.0 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OC(C)(C)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923639 68708 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 3.0 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OC(C)(C)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
56942244 124664 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 124664 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
162648546 179288 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC=O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745666 179288 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC=O)cc1 10.1021/acs.jmedchem.9b02122
58438460 111233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287217 111233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
56926356 68662 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923512 68662 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
56926176 68657 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923505 68657 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
71453390 81417 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164500 81417 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162663952 181560 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 13 2 7 6.6 COc1ccc(/C=C(\C#N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4782383 181560 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 13 2 7 6.6 COc1ccc(/C=C(\C#N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
118725963 116679 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 541 7 1 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394203 116679 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 541 7 1 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
44434112 168283 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL438154 168283 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
3174463 66420 3 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 12 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL185876 66420 3 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 12 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
56926464 68682 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
CHEMBL1923612 68682 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
118725960 116675 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 5 0 6 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
CHEMBL3394199 116675 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 5 0 6 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
162657547 180391 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 694 15 2 9 6.2 COc1ccc(/C=C(\C#N)C(=O)OCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4758721 180391 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 694 15 2 9 6.2 COc1ccc(/C=C(\C#N)C(=O)OCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162658148 180556 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 565 13 4 7 3.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760746 180556 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 565 13 4 7 3.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
162662164 180818 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 12 3 6 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763700 180818 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 12 3 6 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
127047362 139176 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 139176 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
3154000 123738 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 530 12 3 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(O)cc1 10.1021/jm040103i
CHEMBL363467 123738 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 530 12 3 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(O)cc1 10.1021/jm040103i
162651277 179606 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 598 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4749525 179606 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 598 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
3180629 67001 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 518 11 2 3 5.8 CCN(CC)CCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL188582 67001 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 518 11 2 3 5.8 CCN(CC)CCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
44434016 89748 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL238228 89748 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
72190452 91832 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426682 91832 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
118725964 116680 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 7 1 6 4.1 COc1ccc(CCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394204 116680 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 7 1 6 4.1 COc1ccc(CCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
70692600 75506 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048813 75506 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
70682036 75510 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048817 75510 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
70686293 75515 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048822 75515 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
58438460 111233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
CHEMBL3287217 111233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
162660604 180627 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761319 180627 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162671996 182239 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4791255 182239 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
25032438 115683 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human ghrelin receptor by receptor binding assayBinding affinity to human ghrelin receptor by receptor binding assay
ChEMBL 485 14 2 6 3.8 CCN(CC)CCCS(=O)(=O)N[C@H](CCc1ccccc1)c1nc(-c2ccc(OC)cc2)n[nH]1 10.1021/jm5003183
CHEMBL3358450 115683 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human ghrelin receptor by receptor binding assayBinding affinity to human ghrelin receptor by receptor binding assay
ChEMBL 485 14 2 6 3.8 CCN(CC)CCCS(=O)(=O)N[C@H](CCc1ccccc1)c1nc(-c2ccc(OC)cc2)n[nH]1 10.1021/jm5003183
11692516 68691 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923621 68691 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
67407161 91838 0 None 1819 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 467 5 0 5 4.3 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426688 91838 0 None 1819 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 467 5 0 5 4.3 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
67410074 111232 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287216 111232 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
56926782 68700 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923631 68700 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70696687 75505 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048812 75505 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
127046806 139390 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 139390 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127048038 139429 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 139429 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44434076 89333 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
CHEMBL237717 89333 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
56926463 68681 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923611 68681 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
11526696 71243 13 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923502 71243 13 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1963249 71243 13 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
72191051 91816 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 456 5 0 6 3.4 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426666 91816 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 456 5 0 6 3.4 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
58438460 111233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287217 111233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
56926783 68701 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923632 68701 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
162658631 180491 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 561 12 3 7 3.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759983 180491 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 561 12 3 7 3.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#N)cc1 10.1021/acs.jmedchem.9b02122
118725958 116674 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 4 0 7 3.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4nn(C)c5ncccc45)CC3)C2)ncn1 10.1021/ml500414n
CHEMBL3394197 116674 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 4 0 7 3.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4nn(C)c5ncccc45)CC3)C2)ncn1 10.1021/ml500414n
162659337 180724 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 665 15 3 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C#N)Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4762631 180724 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 665 15 3 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C#N)Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
73355325 91821 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN(C(C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426671 91821 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN(C(C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
70696688 75511 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048818 75511 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
127048060 139318 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799222 139318 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
56942388 139400 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 139400 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
162677361 182917 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4799766 182917 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
58438475 91827 0 None 1548 2 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
CHEMBL2426677 91827 0 None 1548 2 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
44434109 145736 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392076 145736 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
134139080 147138 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3931856 147138 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
44434010 88331 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL236311 88331 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
127047655 139071 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 139071 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
44340007 9209 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 541 9 2 6 2.0 CN1N=C2CCN(C(=O)[C@@H](COCc3ccc(F)c(F)c3)NC(=O)C(C)(C)N)CC2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
CHEMBL111026 9209 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 541 9 2 6 2.0 CN1N=C2CCN(C(=O)[C@@H](COCc3ccc(F)c(F)c3)NC(=O)C(C)(C)N)CC2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
56925344 68710 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923641 68710 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
44434083 89586 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL238155 89586 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
44434050 144905 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL391428 144905 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
44396306 66926 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 452 11 2 3 4.7 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC1CCCCC1 10.1021/jm040103i
CHEMBL188173 66926 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 452 11 2 3 4.7 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC1CCCCC1 10.1021/jm040103i
145948725 166925 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299615 166925 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
57345597 70911 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ccc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956988 70911 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ccc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56942243 124663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 124663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
162648837 179248 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745116 179248 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
127048059 139023 0 None - 1 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797225 139023 0 None - 1 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
11526745 68711 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923642 68711 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
57400003 70920 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2ccc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956996 70920 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2ccc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
155529391 170864 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4463042 170864 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
70690449 75503 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048810 75503 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
118725965 116681 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.0 CNC(=O)c1cc(OC)ccc1CC(=O)N1CCC2(CC1)CN([C@@H]1CCc3cc(-c4cc(C)ncn4)ccc31)C2 10.1021/ml500414n
CHEMBL3394205 116681 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.0 CNC(=O)c1cc(OC)ccc1CC(=O)N1CCC2(CC1)CN([C@@H]1CCc3cc(-c4cc(C)ncn4)ccc31)C2 10.1021/ml500414n
44434080 89467 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237933 89467 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
162647450 179281 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 12 2 6 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745548 179281 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 12 2 6 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C)cc1 10.1021/acs.jmedchem.9b02122
71456910 81475 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164823 81475 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
3154005 66425 4 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 550 13 1 4 5.7 CCN(CC)CCCN(C(=O)CCN1CCCc2ccccc21)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL185887 66425 4 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 550 13 1 4 5.7 CCN(CC)CCCN(C(=O)CCN1CCCc2ccccc21)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
70696689 75514 0 None - 1 Human 6.7 pKi = 6.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048821 75514 0 None - 1 Human 6.7 pKi = 6.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
56926681 68694 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923624 68694 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
127047409 139088 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797639 139088 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
56926785 68703 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923634 68703 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70688404 75499 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
CHEMBL2048807 75499 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
44434009 166882 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL429799 166882 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
53248756 60838 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometryInhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 457 5 0 5 5.6 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C)C1 10.1016/j.bmc.2011.02.021
CHEMBL1765654 60838 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometryInhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 457 5 0 5 5.6 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C)C1 10.1016/j.bmc.2011.02.021
CHEMBL2170701 207606 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cn(C)c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
10253999 123263 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 466 12 2 3 5.1 CCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL362303 123263 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 466 12 2 3 5.1 CCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
127048061 139193 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798337 139193 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
162662593 181378 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 591 12 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN2CCC(N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780100 181378 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 591 12 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN2CCC(N)CC2)cc1 10.1021/acs.jmedchem.9b02122
44579909 186310 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489819 186310 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44434073 89156 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL237507 89156 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
70694649 75516 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048823 75516 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
162659161 180799 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763471 180799 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
162652815 179785 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 564 14 2 6 5.3 CCN(CC)CC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4751674 179785 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 564 14 2 6 5.3 CCN(CC)CC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170779 207611 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434008 145989 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL392268 145989 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44434110 88070 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235135 88070 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44577060 187459 0 None -69 7 Human 6.6 pKi = 6.6 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 187459 0 None -69 7 Human 6.6 pKi = 6.6 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL2170780 207612 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
71453404 81477 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164826 81477 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
70692603 75509 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048816 75509 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
56926360 68678 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923608 68678 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
72190451 91830 0 None 524 2 Human 7.6 pKi = 7.6 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426680 91830 0 None 524 2 Human 7.6 pKi = 7.6 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
44579907 186455 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491044 186455 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
73350846 91820 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426670 91820 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
44576247 212441 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
CHEMBL506986 212441 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
44576247 212441 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL506986 212441 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
44579880 186243 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489401 186243 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
118725962 116678 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 526 6 1 7 3.1 COc1cc(C(N)=O)c(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)cn1 10.1021/ml500414n
CHEMBL3394202 116678 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 526 6 1 7 3.1 COc1cc(C(N)=O)c(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)cn1 10.1021/ml500414n
44396384 67056 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 574 14 2 5 6.1 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1 10.1021/jm040103i
CHEMBL188839 67056 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 574 14 2 5 6.1 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1 10.1021/jm040103i
44434074 154123 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL399625 154123 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
70684155 75517 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048824 75517 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
72191050 91817 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 453 4 0 5 4.0 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426667 91817 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 453 4 0 5 4.0 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
72190449 91826 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426676 91826 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
118725966 116682 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.6 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(NC(C)=O)c1 10.1021/ml500414n
CHEMBL3394206 116682 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.6 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(NC(C)=O)c1 10.1021/ml500414n
162675268 182766 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 645 13 3 8 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2(C#N)CCOCC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797685 182766 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 645 13 3 8 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2(C#N)CCOCC2)cc1 10.1021/acs.jmedchem.9b02122
3153999 126297 3 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 494 14 2 3 5.9 CCCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL365489 126297 3 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 494 14 2 3 5.9 CCCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
71451551 81425 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164508 81425 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
72190451 91830 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426680 91830 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
72190451 91830 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426680 91830 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
9950632 88264 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL236038 88264 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
127046472 139151 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798056 139151 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127045859 139156 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798095 139156 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127045859 139156 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798095 139156 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
127047523 139520 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3800422 139520 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
71456897 81424 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164507 81424 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162653916 179953 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753794 179953 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162643920 181188 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4777792 181188 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
155537651 171740 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4475293 171740 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57391292 70919 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 473 6 0 8 4.6 COc1ccc2cccc(Oc3ccc4nc(C)n(C[C@H]5CCCN(C(C)C)C5)c(=O)c4n3)c2n1 10.1016/j.bmcl.2012.01.078
CHEMBL1956995 70919 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 473 6 0 8 4.6 COc1ccc2cccc(Oc3ccc4nc(C)n(C[C@H]5CCCN(C(C)C)C5)c(=O)c4n3)c2n1 10.1016/j.bmcl.2012.01.078
57345598 70928 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 411 5 0 7 3.5 Cc1nc2ncc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957004 70928 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 411 5 0 7 3.5 Cc1nc2ncc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
53373577 91836 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 458 5 0 7 2.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426686 91836 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 458 5 0 7 2.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
57391294 70922 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2cnc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956998 70922 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2cnc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
155526063 170459 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4456830 170459 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
162663004 181457 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 603 13 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C)(C)C#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4781141 181457 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 603 13 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C)(C)C#N)cc1 10.1021/acs.jmedchem.9b02122
155557019 174005 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174005 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
71453489 207613 13 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
CHEMBL2170781 207613 13 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
67405379 91833 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426683 91833 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
25211977 186309 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489818 186309 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
25098836 190852 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519322 190852 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
127047525 139224 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798559 139224 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
162653309 179881 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 718 14 5 8 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4752936 179881 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 718 14 5 8 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44579756 186231 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489370 186231 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
162666964 181918 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 4.6 CCNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4787023 181918 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 4.6 CCNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170693 207598 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434121 89464 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL237927 89464 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
56926584 68690 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 4 3 5 3.2 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923620 68690 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 4 3 5 3.2 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434120 89463 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237926 89463 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
44434007 88133 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235446 88133 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
11541143 68688 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 4 3 5 3.0 CCC[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923618 68688 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 4 3 5 3.0 CCC[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
24969520 68692 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.5 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923622 68692 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.5 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL2170694 207599 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
56926580 68684 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 4 5 3.1 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)NC1=O 10.1021/jm2007062
CHEMBL1923614 68684 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 4 5 3.1 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)NC1=O 10.1021/jm2007062
162653802 179939 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753592 179939 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
73346226 91818 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 487 8 0 7 3.4 COCC(c1ccc(-c2ncccn2)cc1)N1CC2(CCN(C(=O)Cc3ccc(OC)cn3)CC2)C1 10.1016/j.bmcl.2013.07.044
CHEMBL2426668 91818 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 487 8 0 7 3.4 COCC(c1ccc(-c2ncccn2)cc1)N1CC2(CCN(C(=O)Cc3ccc(OC)cn3)CC2)C1 10.1016/j.bmcl.2013.07.044
162674738 182795 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797988 182795 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
56926177 68658 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923506 68658 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
56926581 68685 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 5 4 5 3.4 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm2007062
CHEMBL1923615 68685 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 5 4 5 3.4 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm2007062
71458747 81412 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164494 81412 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
23631116 4037 19 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
3538 4037 19 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
CHEMBL243001 4037 19 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
127046956 139414 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 139414 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
118725961 116676 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 523 6 0 7 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
CHEMBL3394200 116676 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 523 6 0 7 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
162663407 181438 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 562 13 3 6 4.3 C=CC(=O)NCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780843 181438 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 562 13 3 6 4.3 C=CC(=O)NCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
56926462 68680 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923610 68680 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
70695747 72829 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHSR1a receptorDisplacement of [125I]Ghrelin from human GHSR1a receptor
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 72829 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHSR1a receptorDisplacement of [125I]Ghrelin from human GHSR1a receptor
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
67406334 111229 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287213 111229 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
57390496 68698 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 68698 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
71453489 207613 13 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 207613 13 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
56926269 68661 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O 10.1021/jm2007062
CHEMBL1923511 68661 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O 10.1021/jm2007062
56926784 68702 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923633 68702 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70688404 75499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
CHEMBL2048807 75499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
70688404 75499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048807 75499 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
44434123 145005 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
CHEMBL391510 145005 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
56926582 68686 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923616 68686 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
16114404 154346 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL400814 154346 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
25190383 81483 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164831 81483 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
11683187 198240 35 None -457 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to ghrelin receptorBinding affinity to ghrelin receptor
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
CHEMBL594828 198240 35 None -457 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to ghrelin receptorBinding affinity to ghrelin receptor
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
70684154 75501 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048809 75501 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
44434055 88861 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL236858 88861 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
56942385 124665 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 124665 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
56942535 139218 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 139218 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
24180592 96552 0 None -134 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 96552 0 None -134 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
44434113 88207 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235793 88207 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44434051 88971 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237058 88971 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
118725954 116672 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 467 4 0 5 4.3 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
CHEMBL3394193 116672 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 467 4 0 5 4.3 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
24969603 68697 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
CHEMBL1923627 68697 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
57394882 70935 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 447 5 0 9 3.3 Cc1nc2ncc(Oc3ccc4c(c3)ncn4C)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957011 70935 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 447 5 0 9 3.3 Cc1nc2ncc(Oc3ccc4c(c3)ncn4C)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
9876514 9037 2 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 610 10 2 7 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)[C@]2(Cc2ccccn2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL109980 9037 2 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 610 10 2 7 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)[C@]2(Cc2ccccn2)C1 10.1016/s0960-894x(02)00734-5
70682037 75513 14 None 43 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2013.07.044
CHEMBL2048820 75513 14 None 43 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2013.07.044
145948708 166924 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299606 166924 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
67410074 111232 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287216 111232 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
56926465 68683 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O 10.1021/jm2007062
CHEMBL1923613 68683 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O 10.1021/jm2007062
44434119 89462 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
CHEMBL237925 89462 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
70694648 75504 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048811 75504 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
155561671 175081 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4581511 175081 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
56926894 68707 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923638 68707 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
162672372 182494 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 14 3 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4794448 182494 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 14 3 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
56925345 68712 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923643 68712 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
56926464 68682 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923612 68682 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O 10.1021/jm2007062
56942387 139119 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 139119 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL105462 206716 34 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm960054c
56926680 68693 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923623 68693 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
162649014 179351 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4746362 179351 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
162666112 181722 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 13 3 8 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccc(C#N)nc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4784240 181722 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 13 3 8 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccc(C#N)nc2)cc1 10.1021/acs.jmedchem.9b02122
162676229 182712 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797064 182712 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
58438475 91827 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426677 91827 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
58438475 91827 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
CHEMBL2426677 91827 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
56926461 68679 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923609 68679 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
118725956 116673 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 493 5 0 5 4.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(C5CC5)cn4)CC3)C2)ncn1 10.1021/ml500414n
CHEMBL3394195 116673 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 493 5 0 5 4.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(C5CC5)cn4)CC3)C2)ncn1 10.1021/ml500414n
155551597 173367 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4541252 173367 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57394797 70926 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2cnc(Oc3ccc(F)c4cccnc34)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957002 70926 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2cnc(Oc3ccc(F)c4cccnc34)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162649450 179464 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4747770 179464 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
58438464 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
58438464 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 3004 28 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
67406334 111229 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287213 111229 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
57401798 70912 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ncc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956989 70912 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ncc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
58438475 91827 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
CHEMBL2426677 91827 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
11541319 68713 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 3 3 5 2.7 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2O1 10.1021/jm2007062
CHEMBL1923644 68713 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 3 3 5 2.7 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2O1 10.1021/jm2007062
162659375 180759 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 566 14 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCC(=O)O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763077 180759 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 566 14 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCC(=O)O)cc1 10.1021/acs.jmedchem.9b02122
127046807 139397 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 139397 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127047654 139434 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 139434 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
121879 2195 19 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
5868 2195 19 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
CHEMBL308716 2195 19 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
162665952 181787 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4785149 181787 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
134139753 145491 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3918783 145491 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
162663868 181396 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780408 181396 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
56926268 68660 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O 10.1021/jm2007062
CHEMBL1923510 68660 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O 10.1021/jm2007062
56926175 68656 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923504 68656 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
23635235 165937 0 None -239 5 Human 6.2 pKi = 6.2 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL427860 165937 0 None -239 5 Human 6.2 pKi = 6.2 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
70686292 75512 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048819 75512 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
90644554 111231 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ccncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287215 111231 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ccncn5)ccc42)C3)nc1 10.1021/ml400473x
70682037 75513 14 None 43 2 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048820 75513 14 None 43 2 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
11664206 68696 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923626 68696 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
216208 9620 27 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
CHEMBL113313 9620 27 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
56926682 68695 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923625 68695 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
67408128 91834 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 5 0 6 3.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426684 91834 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 5 0 6 3.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
24180646 147638 0 None -1023 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 147638 0 None -1023 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
57390496 68698 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 68698 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL501261 212354 19 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.8b01644
56926892 68705 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923636 68705 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434012 88631 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL236513 88631 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
127046473 139237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798645 139237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
56942099 124661 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 124661 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
66601728 81415 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164499 81415 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162657465 180449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759418 180449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
56926891 68704 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923635 68704 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434015 88049 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL235011 88049 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
67407808 91837 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426687 91837 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
56926173 68655 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923501 68655 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
3153998 67166 3 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 480 13 2 3 5.5 CCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL189561 67166 3 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 480 13 2 3 5.5 CCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
56926893 68706 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
CHEMBL1923637 68706 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
66788278 124659 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 124659 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127045858 139319 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 139319 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
162677268 182981 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4800459 182981 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
58438487 91835 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 497 6 0 6 4.3 CCc1cnc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(OC)cn4)CC3)C2)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426685 91835 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 497 6 0 6 4.3 CCc1cnc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(OC)cn4)CC3)C2)nc1 10.1016/j.bmcl.2013.07.044
67407808 91837 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426687 91837 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
67407808 91837 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426687 91837 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
67406727 116677 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394201 116677 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
162656896 180268 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4757313 180268 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
44579823 183489 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482420 183489 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44396320 66468 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 515 12 2 4 5.4 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccncc1 10.1021/jm040103i
CHEMBL186045 66468 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 515 12 2 4 5.4 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccncc1 10.1021/jm040103i
162674996 182797 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 522 12 3 6 4.2 CNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4798018 182797 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 522 12 3 6 4.2 CNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
44434111 145738 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392077 145738 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
9745 2410 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
9804938 2410 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
CHEMBL278623 2410 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
DB13074 2410 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
9745 2410 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
9804938 2410 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
CHEMBL278623 2410 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
DB13074 2410 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
1102 1289 0 None - 1 Human 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1093 1756 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1756 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1756 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1756 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
1100 1572 41 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
6918297 1572 41 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
CHEMBL108335 1572 41 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
1099 1749 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1749 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1092 3097 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
134715446 3097 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
2232 3097 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
6918245 3097 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL106593 3097 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
58438464 3004 28 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 3004 28 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 3004 28 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 3004 28 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
58438464 3004 28 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 3004 28 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 3004 28 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 3004 28 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
58438464 3004 28 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 3004 28 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 3004 28 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 3004 28 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
12413 3009 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
164946906 3009 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
12413 3009 0 None 3 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
164946906 3009 0 None 3 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
23631116 4037 19 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
3538 4037 19 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
CHEMBL243001 4037 19 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
1098 1359 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1098 1359 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14763915
1101 650 0 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15339248
10740 1899 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 4 1 3 4.4 COc1ccc(c(c1Cl)Cl)[C@@H](NC(=O)N([C@@H]1CCN(CC1(C)C)C)C)C 25327342
146170991 1899 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 4 1 3 4.4 COc1ccc(c(c1Cl)Cl)[C@@H](NC(=O)N([C@@H]1CCN(CC1(C)C)C)C)C 25327342
1092 3097 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
134715446 3097 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
2232 3097 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
6918245 3097 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
CHEMBL106593 3097 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
178024 1932 30 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
5867 1932 30 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
CHEMBL13817 1932 30 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
1099 1749 0 None - 1 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1093 1756 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1756 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793