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
57781216 125313 0 None 8 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648356 125313 0 None 8 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
24954989 1497 1 None 25 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 10.1021/jm200385u
7774 1497 1 None 25 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 10.1021/jm200385u
CHEMBL1802025 1497 1 None 25 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 10.1021/jm200385u
1357 2440 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
1672 2440 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
224 2440 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
896 2440 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
CHEMBL45 2440 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
DB01065 2440 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
1357 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
1672 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
224 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
896 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
CHEMBL45 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
DB01065 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
1357 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
1672 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
224 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
896 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
CHEMBL45 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
DB01065 2440 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
139451757 184238 0 None 3 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 311 6 1 5 2.2 CCOc1nc2cc(Cl)c(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4852096 184238 0 None 3 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 311 6 1 5 2.2 CCOc1nc2cc(Cl)c(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
139451761 184004 0 None 4 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4848885 184004 0 None 4 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
139451781 184265 0 None -2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 289 5 1 5 1.5 CCOc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
CHEMBL4852440 184265 0 None -2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 289 5 1 5 1.5 CCOc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
139451795 184737 0 None 2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 277 6 1 5 1.6 CCOc1nc2ccc(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859677 184737 0 None 2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 277 6 1 5 1.6 CCOc1nc2ccc(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
139451767 184411 0 None 5 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 263 5 1 5 1.2 COc1ccc2nc(OC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4854625 184411 0 None 5 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 263 5 1 5 1.2 COc1ccc2nc(OC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
139451764 185675 0 None -2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 275 4 1 5 1.1 COc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
CHEMBL4873903 185675 0 None -2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 275 4 1 5 1.1 COc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
145981769 166103 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 270 3 1 3 2.4 COc1ccc2ccc3c(c2n1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4281712 166103 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 270 3 1 3 2.4 COc1ccc2ccc3c(c2n1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
139451790 184704 13 None 6 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859295 184704 13 None 6 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
1357 2440 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
1672 2440 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
224 2440 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
896 2440 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
CHEMBL45 2440 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
DB01065 2440 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
1357 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1672 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
224 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
896 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
CHEMBL45 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
DB01065 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1357 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
1672 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
224 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
896 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
CHEMBL45 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
DB01065 2440 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
139451757 184238 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 311 6 1 5 2.2 CCOc1nc2cc(Cl)c(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4852096 184238 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 311 6 1 5 2.2 CCOc1nc2cc(Cl)c(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
139451763 185741 0 None -1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 305 8 1 5 2.4 CCCC(=O)NCCn1c(OCC)nc2ccc(OC)cc21 10.1021/acs.jmedchem.0c00627
CHEMBL4874954 185741 0 None -1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 305 8 1 5 2.4 CCCC(=O)NCCn1c(OCC)nc2ccc(OC)cc21 10.1021/acs.jmedchem.0c00627
9839629 99641 0 None -1 2 Human 9.8 pEC50 = 9.8 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 309 5 1 3 3.8 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL287560 99641 0 None -1 2 Human 9.8 pEC50 = 9.8 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 309 5 1 3 3.8 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
139451761 184004 0 None 4 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4848885 184004 0 None 4 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
198 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
82148 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
99 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
CHEMBL10878 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
DB06594 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
145982070 165911 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 283 3 1 2 3.2 COc1ccc2ccc3c(c2c1)C(C)(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4278248 165911 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 283 3 1 2 3.2 COc1ccc2ccc3c(c2c1)C(C)(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
145993214 166187 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 285 3 2 3 2.2 CNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4283539 166187 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 285 3 2 3 2.2 CNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
139451767 184411 0 None 5 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 263 5 1 5 1.2 COc1ccc2nc(OC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4854625 184411 0 None 5 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 263 5 1 5 1.2 COc1ccc2nc(OC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
139451776 184418 0 None 3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 277 6 1 5 1.6 COc1ccc2nc(OC)n(CCCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4854836 184418 0 None 3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 277 6 1 5 1.6 COc1ccc2nc(OC)n(CCCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
139451799 185247 0 None 3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 279 5 1 5 1.9 COc1ccc2nc(SC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4867553 185247 0 None 3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 279 5 1 5 1.9 COc1ccc2nc(SC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
139451790 184704 13 None 6 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859295 184704 13 None 6 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
164946945 189625 1 None -3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5174929 189625 1 None -3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
139451781 184265 0 None -2 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 289 5 1 5 1.5 CCOc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
CHEMBL4852440 184265 0 None -2 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 289 5 1 5 1.5 CCOc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
139451795 184737 0 None 2 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 277 6 1 5 1.6 CCOc1nc2ccc(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859677 184737 0 None 2 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 277 6 1 5 1.6 CCOc1nc2ccc(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
139451764 185675 0 None -2 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 275 4 1 5 1.1 COc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
CHEMBL4873903 185675 0 None -2 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 275 4 1 5 1.1 COc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
168296374 191910 0 None 9 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
CHEMBL5209359 191910 0 None 9 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
53237951 61675 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 333 5 1 2 3.7 CC(=O)NCCC1=C(Cc2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774518 61675 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 333 5 1 2 3.7 CC(=O)NCCC1=C(Cc2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
168296374 191910 0 None 9 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
CHEMBL5209359 191910 0 None 9 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
44394435 66578 0 None 34 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity towards human Melatonin receptor type 1A was determined by its ability to inhibit forskolin stimulated cAMP accumulationAgonist activity towards human Melatonin receptor type 1A was determined by its ability to inhibit forskolin stimulated cAMP accumulation
ChEMBL 361 8 1 2 5.2 CC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL186586 66578 0 None 34 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity towards human Melatonin receptor type 1A was determined by its ability to inhibit forskolin stimulated cAMP accumulationAgonist activity towards human Melatonin receptor type 1A was determined by its ability to inhibit forskolin stimulated cAMP accumulation
ChEMBL 361 8 1 2 5.2 CC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
168274836 189544 0 None 17 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5173623 189544 0 None 17 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
139451780 185352 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 303 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CC1 10.1021/acs.jmedchem.0c00627
CHEMBL4869463 185352 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 303 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CC1 10.1021/acs.jmedchem.0c00627
137660333 158961 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 244 4 1 3 1.9 COc1ccc2cccc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4102177 158961 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 244 4 1 3 1.9 COc1ccc2cccc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.12.013
145979585 165926 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 313 5 2 3 3.0 CCCNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4278446 165926 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 313 5 2 3 3.0 CCCNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
145986532 166717 0 None -4 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 269 3 1 2 3.0 COc1ccc2ccc3c(c2c1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4293386 166717 0 None -4 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 269 3 1 2 3.0 COc1ccc2ccc3c(c2c1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
122188347 122634 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 232 3 1 2 2.0 CCC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612604 122634 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 232 3 1 2 2.0 CCC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
139451766 183855 0 None -4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 325 7 1 5 2.6 CCOc1nc2cc(Cl)c(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4846505 183855 0 None -4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 325 7 1 5 2.6 CCOc1nc2cc(Cl)c(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
139451769 185550 0 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)CC 10.1021/acs.jmedchem.0c00627
CHEMBL4872217 185550 0 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)CC 10.1021/acs.jmedchem.0c00627
1357 2440 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
1672 2440 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
224 2440 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
896 2440 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
CHEMBL45 2440 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
DB01065 2440 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
127026427 137146 0 None -1 2 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3oc(CNC(=O)C4CC4)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3758679 137146 0 None -1 2 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3oc(CNC(=O)C4CC4)cc3c2c1 10.1016/j.ejmech.2015.12.047
127026425 137282 0 None 8 2 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3occ(CNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759816 137282 0 None 8 2 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3occ(CNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
168274836 189544 0 None 17 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5173623 189544 0 None 17 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
198 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
82148 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
99 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
CHEMBL10878 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
DB06594 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
198 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
198 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
82148 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
82148 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
99 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
99 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
CHEMBL10878 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
CHEMBL10878 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
DB06594 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
DB06594 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
1357 2440 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
1672 2440 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
224 2440 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
896 2440 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
CHEMBL45 2440 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
DB01065 2440 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
198 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
82148 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
99 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
CHEMBL10878 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
DB06594 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
198 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
82148 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
99 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
CHEMBL10878 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
DB06594 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
198 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
82148 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
99 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
CHEMBL10878 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
DB06594 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
122188346 122633 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 262 4 1 3 2.0 CCC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612603 122633 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 262 4 1 3 2.0 CCC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
139451776 184418 0 None 3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 277 6 1 5 1.6 COc1ccc2nc(OC)n(CCCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4854836 184418 0 None 3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 277 6 1 5 1.6 COc1ccc2nc(OC)n(CCCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
1357 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
1672 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
224 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
896 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
CHEMBL45 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
DB01065 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
18360658 8787 0 None 10 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 518 13 2 5 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4scc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1097497 8787 0 None 10 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 518 13 2 5 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4scc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
145979282 166111 0 None -1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4281915 166111 0 None -1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145986700 166655 0 None -5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 328 4 2 2 3.5 CCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4292109 166655 0 None -5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 328 4 2 2 3.5 CCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
122220128 159116 0 None -27 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 309 6 2 3 2.3 COc1ccc2cccc(C(CO)CNC(=O)C(F)F)c2c1 10.1039/C4MD00149D
CHEMBL4104020 159116 0 None -27 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 309 6 2 3 2.3 COc1ccc2cccc(C(CO)CNC(=O)C(F)F)c2c1 10.1039/C4MD00149D
145992795 166227 0 None -25 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 342 5 2 2 3.9 CCCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4284223 166227 0 None -25 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 342 5 2 2 3.9 CCCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145991111 166348 0 None -10 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 319 5 1 3 2.8 CCS(=O)(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4286494 166348 0 None -10 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 319 5 1 3 2.8 CCS(=O)(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
23658143 155824 1 None -41 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
CHEMBL4066279 155824 1 None -41 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
46888492 8740 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 564 14 2 5 6.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)c5ccco5)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1096991 8740 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 564 14 2 5 6.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)c5ccco5)c4c3)cc12 10.1016/j.bmc.2010.04.008
122188231 122619 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 247 3 2 2 1.8 CCNC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612462 122619 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 247 3 2 2 1.8 CCNC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
19703063 28687 1 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1016/j.bmcl.2011.02.097
CHEMBL137969 28687 1 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1016/j.bmcl.2011.02.097
46888520 8541 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 538 15 2 4 6.1 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095195 8541 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 538 15 2 4 6.1 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
21581654 60413 1 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760944 60413 1 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
10385056 111731 0 None -354 2 Human 6.9 pEC50 = 6.9 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 379 9 1 4 4.3 C=CCC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL329086 111731 0 None -354 2 Human 6.9 pEC50 = 6.9 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 379 9 1 4 4.3 C=CCC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm0005252
164946945 189625 1 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5174929 189625 1 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
145986330 166493 0 None -3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 286 3 2 2 2.7 COc1ccc2ccc3c(c2c1)C(CNC(N)=S)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4289115 166493 0 None -3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 286 3 2 2 2.7 COc1ccc2ccc3c(c2c1)C(CNC(N)=S)CC3 10.1016/j.ejmech.2017.10.025
52918080 60425 0 None -12 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 287 4 1 4 2.1 COc1ccc2c3c(n(CCNC(C)=O)c2n1)CCCC3 10.1016/j.bmcl.2011.02.097
CHEMBL1760957 60425 0 None -12 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 287 4 1 4 2.1 COc1ccc2c3c(n(CCNC(C)=O)c2n1)CCCC3 10.1016/j.bmcl.2011.02.097
9937825 8765 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 564 17 2 4 6.7 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)CC=C)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1097315 8765 0 None 2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 564 17 2 4 6.7 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)CC=C)c4c3)cc12 10.1016/j.bmc.2010.04.008
71508233 86632 0 None -676 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 355 10 1 3 3.9 CCC(=O)NCCCc1cc(OC)ccc1CCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326201 86632 0 None -676 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 355 10 1 3 3.9 CCC(=O)NCCCc1cc(OC)ccc1CCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
122188230 122618 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 277 4 2 3 1.8 CCNC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612461 122618 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 277 4 2 3 1.8 CCNC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
137639112 156298 0 None -8128 2 Human 5.8 pEC50 = 5.8 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 245 4 2 3 1.5 COc1ccc2cccc(CCNC(N)=O)c2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4071572 156298 0 None -8128 2 Human 5.8 pEC50 = 5.8 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 245 4 2 3 1.5 COc1ccc2cccc(CCNC(N)=O)c2n1 10.1016/j.ejmech.2016.12.013
4018512 42959 37 None -2 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 308 5 2 2 3.5 COc1ccc2[nH]c(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1039/d2md00156j
CHEMBL15060 42959 37 None -2 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 308 5 2 2 3.5 COc1ccc2[nH]c(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1039/d2md00156j
121231413 3834 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2c(N1Cc1ccccc1)cccc2OC 10.1021/acs.jmedchem.5b01066
9226 3834 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2c(N1Cc1ccccc1)cccc2OC 10.1021/acs.jmedchem.5b01066
CHEMBL3612464 3834 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2c(N1Cc1ccccc1)cccc2OC 10.1021/acs.jmedchem.5b01066
52953165 62064 0 None -87 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 389 7 1 3 5.6 C=CCC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779810 62064 0 None -87 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 389 7 1 3 5.6 C=CCC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
137647756 157389 0 None -213 2 Human 7.7 pEC50 = 7.7 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 259 4 2 3 1.7 CNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4084612 157389 0 None -213 2 Human 7.7 pEC50 = 7.7 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 259 4 2 3 1.7 CNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
23658146 156564 1 None -15 2 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
CHEMBL4074895 156564 1 None -15 2 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
122188237 122625 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 294 4 1 2 3.1 CC(=O)NC[C@H]1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612469 122625 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 294 4 1 2 3.1 CC(=O)NC[C@H]1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
145981162 165933 0 None -2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 270 3 2 2 2.5 COc1ccc2ccc3c(c2c1)C(CNC(N)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4278575 165933 0 None -2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 270 3 2 2 2.5 COc1ccc2ccc3c(c2c1)C(CNC(N)=O)CC3 10.1016/j.ejmech.2017.10.025
122188349 122636 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 246 4 1 2 2.4 CCCN1c2ccccc2CCC1CNC(C)=O 10.1021/acs.jmedchem.5b01066
CHEMBL3612606 122636 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 246 4 1 2 2.4 CCCN1c2ccccc2CCC1CNC(C)=O 10.1021/acs.jmedchem.5b01066
52918079 60416 0 None -2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 261 6 1 4 2.0 CCCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
CHEMBL1760947 60416 0 None -2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 261 6 1 4 2.0 CCCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
139451766 183855 0 None -4 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 325 7 1 5 2.6 CCOc1nc2cc(Cl)c(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4846505 183855 0 None -4 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 325 7 1 5 2.6 CCOc1nc2cc(Cl)c(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
1357 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
1672 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
224 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
896 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
CHEMBL45 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
DB01065 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
1357 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
1672 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
224 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
896 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
CHEMBL45 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
DB01065 2440 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
10163052 8421 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 483 12 2 4 5.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc(-c4ccc(CO)cc4)cc3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1094212 8421 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 483 12 2 4 5.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc(-c4ccc(CO)cc4)cc3)cc12 10.1016/j.bmc.2010.04.008
46888491 8568 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 501 13 3 4 4.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4[nH]cc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095522 8568 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 501 13 3 4 4.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4[nH]cc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
9870683 8786 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 502 13 2 5 5.2 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4occ(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1097496 8786 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 502 13 2 5 5.2 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4occ(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
46888521 8542 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 499 12 1 5 5.6 COC(=O)Cc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095196 8542 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 499 12 1 5 5.6 COC(=O)Cc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
71508235 86633 0 None -14 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 327 8 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1-c1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326203 86633 0 None -14 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 327 8 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1-c1cccc(OC)c1 10.1016/j.bmc.2012.10.060
145990308 166468 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 328 5 2 2 3.8 CCCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4288690 166468 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 328 5 2 2 3.8 CCCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145987794 166556 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 298 4 2 2 3.2 CCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4290302 166556 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 298 4 2 2 3.2 CCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137637884 155693 0 None -19 2 Human 7.7 pEC50 = 7.7 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 280 3 1 2 3.3 CCC(=O)NC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4064813 155693 0 None -19 2 Human 7.7 pEC50 = 7.7 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 280 3 1 2 3.3 CCC(=O)NC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
53231366 62057 0 None -309 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 363 5 1 3 5.0 CC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779804 62057 0 None -309 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 363 5 1 3 5.0 CC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
86273228 120793 0 None -18 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 258 6 2 2 2.4 C=CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580910 120793 0 None -18 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 258 6 2 2 2.4 C=CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
9927219 111817 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL329263 111817 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
46888522 8543 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 513 12 1 5 6.2 COC(=O)C(C)c1ccc2cc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)ccc2c1 10.1016/j.bmc.2010.04.008
CHEMBL1095197 8543 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 513 12 1 5 6.2 COC(=O)C(C)c1ccc2cc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)ccc2c1 10.1016/j.bmc.2010.04.008
168283863 190366 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 274 3 0 4 2.5 COc1cc2c(CN3CCN(C)CC3)coc2cc1C 10.1039/d2md00156j
CHEMBL5186032 190366 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 274 3 0 4 2.5 COc1cc2c(CN3CCN(C)CC3)coc2cc1C 10.1039/d2md00156j
46845151 8563 0 None 7 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 499 12 2 4 6.1 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cc(C(C)C(=O)O)ccc4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095505 8563 0 None 7 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 499 12 2 4 6.1 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cc(C(C)C(=O)O)ccc4c3)cc12 10.1016/j.bmc.2010.04.008
53231465 62056 0 None -35 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 237 3 1 2 2.7 CC(=O)NCCc1csc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779803 62056 0 None -35 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 237 3 1 2 2.7 CC(=O)NCCc1csc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
122188225 122614 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 218 3 2 2 1.9 CCC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612456 122614 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 218 3 2 2 1.9 CCC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
122188227 122616 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 233 3 3 2 1.7 CCNC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612458 122616 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 233 3 3 2 1.7 CCNC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
10926138 206228 0 None -147 2 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 349 8 1 3 4.3 C=CCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL97186 206228 0 None -147 2 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 349 8 1 3 4.3 C=CCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
23642307 158337 1 None -39 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc(C(CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
CHEMBL4095334 158337 1 None -39 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc(C(CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
145 140 48 None -144 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1832 140 48 None -144 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
CHEMBL7257 140 48 None -144 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
DB14010 140 48 None -144 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
9064 104727 90 None 1 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate ReaderAgonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate Reader
ChEMBL 290 1 5 6 1.5 Oc1cc(O)c2c(c1)O[C@H](c1ccc(O)c(O)c1)[C@@H](O)C2 10.1016/j.ejmech.2020.112960
CHEMBL311498 104727 90 None 1 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate ReaderAgonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate Reader
ChEMBL 290 1 5 6 1.5 Oc1cc(O)c2c(c1)O[C@H](c1ccc(O)c(O)c1)[C@@H](O)C2 10.1016/j.ejmech.2020.112960
7778 799 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 10.1016/j.bmc.2010.04.008
9957516 799 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 10.1016/j.bmc.2010.04.008
CHEMBL1094546 799 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 10.1016/j.bmc.2010.04.008
86079062 180140 0 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 245 4 1 4 1.3 COc1ccc2ncnc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4755860 180140 0 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 245 4 1 4 1.3 COc1ccc2ncnc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
198 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
82148 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
99 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
CHEMBL10878 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
DB06594 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
122188229 122617 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 249 3 3 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612460 122617 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 249 3 3 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
86273227 120790 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 242 4 2 2 1.5 C#CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580907 120790 0 None -3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 242 4 2 2 1.5 C#CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
127025783 137200 0 None -8 2 Human 7.5 pEC50 = 7.5 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3occ(CNC(=O)CF)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759160 137200 0 None -8 2 Human 7.5 pEC50 = 7.5 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3occ(CNC(=O)CF)c3c2c1 10.1016/j.ejmech.2015.12.047
145982333 165993 0 None -2 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4279639 165993 0 None -2 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
53238410 61684 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 361 5 1 2 4.7 CC(=O)NCCC1=C(c2cccc(C(C)C)c2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774529 61684 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 361 5 1 2 4.7 CC(=O)NCCC1=C(c2cccc(C(C)C)c2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
18007928 8562 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 485 12 2 4 5.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CC(=O)O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095504 8562 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 485 12 2 4 5.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CC(=O)O)c4c3)cc12 10.1016/j.bmc.2010.04.008
139451784 184803 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 317 7 1 5 2.4 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CCC1 10.1021/acs.jmedchem.0c00627
CHEMBL4860729 184803 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 317 7 1 5 2.4 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CCC1 10.1021/acs.jmedchem.0c00627
145993566 166806 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 312 5 2 2 3.6 CCCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4294790 166806 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 312 5 2 2 3.6 CCCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137650826 156951 0 None -28 2 Human 7.5 pEC50 = 7.5 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 289 5 2 3 2.3 CCNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4079699 156951 0 None -28 2 Human 7.5 pEC50 = 7.5 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 289 5 2 3 2.3 CCNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
122188236 122624 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 294 4 1 2 3.1 CC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612468 122624 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 294 4 1 2 3.1 CC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
54581170 60424 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 359 4 1 4 1.8 COc1ccc2c(I)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760956 60424 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 359 4 1 4 1.8 COc1ccc2c(I)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
162649247 179485 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 351 6 1 5 3.0 COc1cccc(-c2nc(CCNC(C)=O)c3cc(OC)ccc3n2)c1 10.1016/j.ejmech.2020.112078
CHEMBL4747996 179485 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 351 6 1 5 3.0 COc1cccc(-c2nc(CCNC(C)=O)c3cc(OC)ccc3n2)c1 10.1016/j.ejmech.2020.112078
122178509 120801 0 None -9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580919 120801 0 None -9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1021/acs.jmedchem.5b00245
122188235 122623 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 308 5 1 2 3.5 CCC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612467 122623 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 308 5 1 2 3.5 CCC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
1353 3368 3 None -51 2 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
9998187 3368 3 None -51 2 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
CHEMBL33549 3368 3 None -51 2 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
86273226 120791 0 None -12 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 256 5 2 2 1.9 C#CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580908 120791 0 None -12 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 256 5 2 2 1.9 C#CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
23658145 156909 1 None -52 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
CHEMBL4079214 156909 1 None -52 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
122188232 122620 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 353 6 2 3 3.3 CCNC(=O)NCC1CCc2c(OC)cccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612463 122620 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 353 6 2 3 3.3 CCNC(=O)NCC1CCc2c(OC)cccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
145982167 166047 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 305 4 1 3 2.4 COc1ccc2ccc3c(c2c1)C(CNS(C)(=O)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4280601 166047 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 305 4 1 3 2.4 COc1ccc2ccc3c(c2c1)C(CNS(C)(=O)=O)CC3 10.1016/j.ejmech.2017.10.025
52918077 60414 2 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 233 4 1 4 1.2 COc1ccc2ccn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760945 60414 2 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 233 4 1 4 1.2 COc1ccc2ccn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
53238181 919 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 339 5 1 2 4.4 CC(=O)NCCC1=C(CC2CCCCC2)Cc2c1c1CCOc1cc2 10.1021/jm200221q
7780 919 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 339 5 1 2 4.4 CC(=O)NCCC1=C(CC2CCCCC2)Cc2c1c1CCOc1cc2 10.1021/jm200221q
CHEMBL1774519 919 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 339 5 1 2 4.4 CC(=O)NCCC1=C(CC2CCCCC2)Cc2c1c1CCOc1cc2 10.1021/jm200221q
127026423 137281 0 None -6 2 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 283 4 1 3 3.3 COc1ccc2ccc3occ(CCNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759802 137281 0 None -6 2 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 283 4 1 3 3.3 COc1ccc2ccc3occ(CCNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
127029516 137096 0 None -3 2 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3occ(CNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3758225 137096 0 None -3 2 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3occ(CNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
71508234 696 0 None -173 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 341 9 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1Cc1cccc(c1)OC 10.1016/j.bmc.2012.10.060
7924 696 0 None -173 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 341 9 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1Cc1cccc(c1)OC 10.1016/j.bmc.2012.10.060
CHEMBL2326202 696 0 None -173 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 341 9 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1Cc1cccc(c1)OC 10.1016/j.bmc.2012.10.060
162668689 182166 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 285 5 1 4 2.2 COc1ccc2nc(C3CC3)nc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4790145 182166 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 285 5 1 4 2.2 COc1ccc2nc(C3CC3)nc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
162656758 180330 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 259 5 1 4 1.7 CCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
CHEMBL4757920 180330 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 259 5 1 4 1.7 CCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
10301190 8465 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 511 12 1 5 6.2 COC(=O)c1ccc(-c2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc2)cc1 10.1016/j.bmc.2010.04.008
CHEMBL1094545 8465 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 511 12 1 5 6.2 COC(=O)c1ccc(-c2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc2)cc1 10.1016/j.bmc.2010.04.008
23642306 158515 1 None -17 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 6 2 3 2.5 CCC(=O)NCC(CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
CHEMBL4097233 158515 1 None -17 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 6 2 3 2.5 CCC(=O)NCC(CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
10925526 111829 0 None -47 2 Human 6.3 pEC50 = 6.3 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 329 6 1 3 4.2 COc1ccc2oc(CC3CCCCC3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL329299 111829 0 None -47 2 Human 6.3 pEC50 = 6.3 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 329 6 1 3 4.2 COc1ccc2oc(CC3CCCCC3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
145982333 165993 0 None -2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4279639 165993 0 None -2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145990662 166365 0 None -16 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 312 4 2 2 3.4 CCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4286896 166365 0 None -16 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 312 4 2 2 3.4 CCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145988741 166672 0 None -12 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 299 5 1 3 2.6 COCC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4292336 166672 0 None -12 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 299 5 1 3 2.6 COCC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
52918078 60415 0 None -3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 247 5 1 4 1.6 CCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
CHEMBL1760946 60415 0 None -3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 247 5 1 4 1.6 CCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
127026426 137262 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 309 5 1 3 3.7 COc1ccc2ccc3occ(CCNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759606 137262 0 None -1 2 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 309 5 1 3 3.7 COc1ccc2ccc3occ(CCNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
86273229 120792 1 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 244 5 2 2 2.0 C=CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580909 120792 1 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 244 5 2 2 2.0 C=CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
145979689 166059 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 314 3 2 2 3.1 CNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4280791 166059 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 314 3 2 2 3.1 CNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
122188351 122637 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 294 4 1 2 3.7 CCC(=O)NCC1CCc2ccccc2N1c1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612608 122637 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 294 4 1 2 3.7 CCC(=O)NCC1CCc2ccccc2N1c1ccccc1 10.1021/acs.jmedchem.5b01066
137650611 156958 0 None -91 2 Human 7.2 pEC50 = 7.2 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 244 4 1 3 1.9 CNC(=O)CCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4079784 156958 0 None -91 2 Human 7.2 pEC50 = 7.2 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 244 4 1 3 1.9 CNC(=O)CCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
162649850 179548 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
CHEMBL4748822 179548 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
127026062 137151 0 None -7 2 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3oc(CNC(C)=O)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3758717 137151 0 None -7 2 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3oc(CNC(C)=O)cc3c2c1 10.1016/j.ejmech.2015.12.047
18360631 8612 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 516 13 2 4 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4c(c3)C(CCNC(C)=O)CCC4)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095831 8612 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 516 13 2 4 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4c(c3)C(CCNC(C)=O)CCC4)cc12 10.1016/j.bmc.2010.04.008
145983175 165867 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 314 4 2 2 3.4 CCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4277390 165867 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 314 4 2 2 3.4 CCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
86273222 120796 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 243 3 1 4 2.5 COc1ccc2[nH]cc(Cc3nc(C)no3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580913 120796 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 243 3 1 4 2.5 COc1ccc2[nH]cc(Cc3nc(C)no3)c2c1 10.1021/acs.jmedchem.5b00245
44359437 29671 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 273 5 2 3 2.1 COc1ccc2cccc(C(CO)CNC(C)=O)c2c1 10.1039/C4MD00149D
CHEMBL138807 29671 0 None 3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 273 5 2 3 2.1 COc1ccc2cccc(C(CO)CNC(C)=O)c2c1 10.1039/C4MD00149D
1355 3371 3 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
9806449 3371 3 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
CHEMBL14453 3371 3 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
127025786 137311 0 None -12 2 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 312 5 2 3 3.5 CCNC(=O)NCCc1coc2ccc3ccc(OC)cc3c12 10.1016/j.ejmech.2015.12.047
CHEMBL3760044 137311 0 None -12 2 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 312 5 2 3 3.5 CCNC(=O)NCCc1coc2ccc3ccc(OC)cc3c12 10.1016/j.ejmech.2015.12.047
23658144 157622 1 None -100 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
CHEMBL4087633 157622 1 None -100 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayPartial agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
145979282 166111 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4281915 166111 0 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
127025782 137193 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 297 4 1 3 3.9 COc1ccc2ccc3occ(CNC(=O)C(C)C)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759054 137193 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 297 4 1 3 3.9 COc1ccc2ccc3occ(CNC(=O)C(C)C)c3c2c1 10.1016/j.ejmech.2015.12.047
71508232 86631 0 None -75 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 351 7 1 3 3.6 CCC(=O)NCCCc1cc(OC)ccc1C#Cc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326200 86631 0 None -75 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 351 7 1 3 3.6 CCC(=O)NCCCc1cc(OC)ccc1C#Cc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
122188352 122638 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 263 3 2 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612609 122638 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 263 3 2 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
145988269 166626 0 None -12 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 326 5 2 2 3.8 CCCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4291381 166626 0 None -12 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 326 5 2 2 3.8 CCCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
46865422 86629 0 None -181 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326199 86629 0 None -181 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assayAgonist activity at human MT1 receptor expressed in CHO cells coexpressing Galpha protein 16z25 assessed as increase in calcium mobilization measured for 3 mins by FLIPR assay
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
18007985 8613 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 538 14 2 4 6.0 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C5CC5)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095832 8613 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 538 14 2 4 6.0 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C5CC5)c4c3)cc12 10.1016/j.bmc.2010.04.008
127025784 137195 0 None -8 2 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3oc(CNC(=O)CF)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759084 137195 0 None -8 2 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3oc(CNC(=O)CF)cc3c2c1 10.1016/j.ejmech.2015.12.047
137636213 155533 0 None -47 2 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 273 5 2 3 2.1 CCNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4062947 155533 0 None -47 2 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 273 5 2 3 2.1 CCNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
137655238 158327 0 None -891 2 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 275 4 2 3 1.9 CNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4095210 158327 0 None -891 2 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 275 4 2 3 1.9 CNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
122188224 122613 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 248 4 2 3 1.9 CCC(=O)NCC1CCc2c(cccc2OC)N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612455 122613 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Intrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor transfected in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 248 4 2 3 1.9 CCC(=O)NCC1CCc2c(cccc2OC)N1 10.1021/acs.jmedchem.5b01066
3525815 73783 3 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at MT1Agonist activity at MT1
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2022867 73783 3 None -4 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at MT1Agonist activity at MT1
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
54582195 60423 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 329 5 1 5 1.9 COc1ccc2c(C(=O)C(F)(F)F)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760955 60423 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 329 5 1 5 1.9 COc1ccc2c(C(=O)C(F)(F)F)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
81689735 120798 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 257 4 1 4 2.7 COc1ccc2[nH]cc(CCc3nnc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580916 120798 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 257 4 1 4 2.7 COc1ccc2[nH]cc(CCc3nnc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
86273223 120794 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 242 3 1 3 3.1 COc1ccc2[nH]cc(Cc3ncc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580911 120794 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 242 3 1 3 3.1 COc1ccc2[nH]cc(Cc3ncc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
44241665 194017 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 329 6 1 4 2.6 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCN(C)C2 10.1016/j.bmc.2009.04.068
CHEMBL556908 194017 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 329 6 1 4 2.6 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCN(C)C2 10.1016/j.bmc.2009.04.068
90655902 110365 0 None - 0 Human 9.7 pKi = 9.7 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 330 5 2 4 2.5 CCOC(=O)c1[nH]c2ccc(OC)c3c2c1[C@@H](CNC(C)=O)CC3 10.1021/jm401343c
CHEMBL3260982 110365 0 None - 0 Human 9.7 pKi = 9.7 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 330 5 2 4 2.5 CCOC(=O)c1[nH]c2ccc(OC)c3c2c1[C@@H](CNC(C)=O)CC3 10.1021/jm401343c
24763223 214 0 None - 0 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1021/jm401343c
8289 214 0 None - 0 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1021/jm401343c
CHEMBL3260987 214 0 None - 0 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1021/jm401343c
52918077 60414 2 None -1 2 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 233 4 1 4 1.2 COc1ccc2ccn(CCNC(C)=O)c2n1 10.1021/jm401343c
CHEMBL1760945 60414 2 None -1 2 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by [35S]GTPgamma binding assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by [35S]GTPgamma binding assay
ChEMBL 233 4 1 4 1.2 COc1ccc2ccn(CCNC(C)=O)c2n1 10.1021/jm401343c
11185529 3839 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assayAntagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm401343c
7772 3839 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assayAntagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm401343c
CHEMBL189449 3839 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assayAntagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm401343c
1357 2440 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
103828029 3844 0 None -20 2 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 292 4 1 3 3.5 COc1ccc(c(c1)CNc1cccnc1)Br 32040955
10667 3844 0 None -20 2 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 292 4 1 3 3.5 COc1ccc(c(c1)CNc1cccnc1)Br 32040955
10666 3845 0 None 21 2 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 4 2 3 4.5 Clc1ccc(c(c1)Br)CNc1cccc(c1)c1nnc[nH]1 32040955
138993662 3845 0 None 21 2 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 4 2 3 4.5 Clc1ccc(c(c1)Br)CNc1cccc(c1)c1nnc[nH]1 32040955
10665 3843 0 None 50 2 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 3 4.2 CC(c1ccc(cc1)CNc1cccc(c1)c1[nH]cnn1)C 32040955
137977202 3843 0 None 50 2 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 3 4.2 CC(c1ccc(cc1)CNc1cccc(c1)c1[nH]cnn1)C 32040955
23581869 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None
7712 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None
CHEMBL1783282 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None
DB13994 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None




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
10440 2632 15 None -21 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2632 15 None -21 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2632 15 None -21 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
122178509 120801 0 None -8 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant melatonin receptor-1 expressed in CHO cells assessed as effect on impedance by cellular dielectric spectroscopyAgonist activity at human recombinant melatonin receptor-1 expressed in CHO cells assessed as effect on impedance by cellular dielectric spectroscopy
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580919 120801 0 None -8 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human recombinant melatonin receptor-1 expressed in CHO cells assessed as effect on impedance by cellular dielectric spectroscopyAgonist activity at human recombinant melatonin receptor-1 expressed in CHO cells assessed as effect on impedance by cellular dielectric spectroscopy
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1021/acs.jmedchem.5b00245
19703003 30735 0 None - 0 Human 10.9 pIC50 = 10.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 309 5 2 3 2.9 COc1c[nH]c2nc(-c3ccccc3)c(CCNC(C)=O)c-2c1 10.1021/jm980026p
CHEMBL139855 30735 0 None - 0 Human 10.9 pIC50 = 10.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 309 5 2 3 2.9 COc1c[nH]c2nc(-c3ccccc3)c(CCNC(C)=O)c-2c1 10.1021/jm980026p
9927219 111817 0 None -25 2 Human 10.8 pIC50 = 10.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL329263 111817 0 None -25 2 Human 10.8 pIC50 = 10.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm980026p
57781211 125318 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 376 8 1 3 4.9 CC(=O)NCCC1CCc2ccc3nc(CCCCc4ccccc4)oc3c21 nan
CHEMBL3648361 125318 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 376 8 1 3 4.9 CC(=O)NCCC1CCc2ccc3nc(CCCCc4ccccc4)oc3c21 nan
23634404 125316 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 3.1 CCC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 nan
CHEMBL3648359 125316 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 3.1 CCC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 nan
23725569 125320 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 3 1 3 3.2 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)sc3c21 nan
CHEMBL3648363 125320 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 3 1 3 3.2 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)sc3c21 nan
57781216 125313 0 None 2 2 Human 10.2 pIC50 = 10.2 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 nan
CHEMBL3648356 125313 0 None 2 2 Human 10.2 pIC50 = 10.2 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 nan
23725512 125310 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 256 3 1 3 2.6 CC(=O)NCCC1=CCc2ccc3nc(C)oc3c21 nan
CHEMBL3648350 125310 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 256 3 1 3 2.6 CC(=O)NCCC1=CCc2ccc3nc(C)oc3c21 nan
57781262 160277 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 374 7 1 3 4.9 CC(=O)NC/C=C1\CCc2ccc3nc(CCCCc4ccccc4)oc3c21 nan
CHEMBL4114715 160277 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 374 7 1 3 4.9 CC(=O)NC/C=C1\CCc2ccc3nc(CCCCc4ccccc4)oc3c21 nan
57781258 125326 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 312 3 1 3 3.2 Cc1nc2ccc3c(c2o1)C(CCNC(=O)C(F)(F)F)CC3 nan
CHEMBL3648369 125326 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 312 3 1 3 3.2 Cc1nc2ccc3c(c2o1)C(CCNC(=O)C(F)(F)F)CC3 nan
1357 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.03.006
1672 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.03.006
224 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.03.006
896 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.03.006
CHEMBL45 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.03.006
DB01065 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.03.006
1357 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.11.014
1672 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.11.014
224 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.11.014
896 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.11.014
CHEMBL45 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.11.014
DB01065 2440 133 None -1 9 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2016.11.014
23725514 125315 0 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 3.1 CCC(=O)NCCC1CCc2ccc3nc(C)oc3c21 nan
CHEMBL3648358 125315 0 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 3.1 CCC(=O)NCCC1CCc2ccc3nc(C)oc3c21 nan
23725565 125312 0 None 1 2 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 258 3 1 3 2.7 CC(=O)NCCC1CCc2ccc3nc(C)oc3c21 nan
CHEMBL3648355 125312 0 None 1 2 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 258 3 1 3 2.7 CC(=O)NCCC1CCc2ccc3nc(C)oc3c21 nan
23725567 125319 0 None 2 2 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 3 1 3 3.2 CC(=O)NCCC1CCc2ccc3nc(C)sc3c21 nan
CHEMBL3648362 125319 0 None 2 2 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 3 1 3 3.2 CC(=O)NCCC1CCc2ccc3nc(C)sc3c21 nan
15340632 9667 1 None - 0 Human 9.8 pIC50 = 9.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 267 3 1 2 2.9 CC(=O)NCCc1cccc2ccc3c(c12)C=CCO3 10.1021/jm980026p
CHEMBL11356 9667 1 None - 0 Human 9.8 pIC50 = 9.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 267 3 1 2 2.9 CC(=O)NCCc1cccc2ccc3c(c12)C=CCO3 10.1021/jm980026p
72548703 161007 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]NDP-alpha -MSH from human recombinant MT1 receptor after 240 mins by scintillation counting analysisDisplacement of [125I]NDP-alpha -MSH from human recombinant MT1 receptor after 240 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161007 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]NDP-alpha -MSH from human recombinant MT1 receptor after 240 mins by scintillation counting analysisDisplacement of [125I]NDP-alpha -MSH from human recombinant MT1 receptor after 240 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
1357 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
1672 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
224 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
896 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
CHEMBL45 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
DB01065 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
57781280 160405 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 2 1 3 3.1 CC(=O)NC/C=C1\CCc2ccc3nc(C)sc3c21 nan
CHEMBL4115681 160405 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 2 1 3 3.1 CC(=O)NC/C=C1\CCc2ccc3nc(C)sc3c21 nan
1357 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.010
1672 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.010
224 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.010
896 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.010
CHEMBL45 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.010
DB01065 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.010
1357 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.03.036
1672 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.03.036
224 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.03.036
896 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.03.036
CHEMBL45 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.03.036
DB01065 2440 133 None -1 9 Human 9.7 pIC50 = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.03.036
57781261 125325 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 284 4 1 3 3.1 Cc1nc2ccc3c(c2o1)C(CCNC(=O)C1CC1)CC3 nan
CHEMBL3648368 125325 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 284 4 1 3 3.1 Cc1nc2ccc3c(c2o1)C(CCNC(=O)C1CC1)CC3 nan
57781244 160274 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 270 3 1 3 3.0 CCC(=O)NC/C=C1\CCc2ccc3nc(C)oc3c21 nan
CHEMBL4114700 160274 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 270 3 1 3 3.0 CCC(=O)NC/C=C1\CCc2ccc3nc(C)oc3c21 nan
15340633 97764 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 3 1 2 2.8 CC(=O)NCCc1cccc2ccc3c(c12)CCCO3 10.1021/jm980026p
CHEMBL274358 97764 1 None - 0 Human 9.6 pIC50 = 9.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 3 1 2 2.8 CC(=O)NCCc1cccc2ccc3c(c12)CCCO3 10.1021/jm980026p
15289276 116274 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 347 6 1 3 3.8 COc1ccc2cc(C(=O)c3ccccc3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL337764 116274 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 347 6 1 3 3.8 COc1ccc2cc(C(=O)c3ccccc3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
57781268 160271 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 256 2 1 3 2.6 CC(=O)NC/C=C1\CCc2ccc3nc(C)oc3c21 nan
CHEMBL4114658 160271 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 256 2 1 3 2.6 CC(=O)NC/C=C1\CCc2ccc3nc(C)oc3c21 nan
23725515 125322 0 None -1 2 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 2.9 CCc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 nan
CHEMBL3648365 125322 0 None -1 2 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 2.9 CCc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 nan
1357 2440 133 None -1 9 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
1672 2440 133 None -1 9 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
224 2440 133 None -1 9 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
896 2440 133 None -1 9 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
CHEMBL45 2440 133 None -1 9 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
DB01065 2440 133 None -1 9 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
1357 2440 133 None -1 9 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human ML1A receptor by radioligand displacement assayBinding affinity to human ML1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2013.03.016
1672 2440 133 None -1 9 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human ML1A receptor by radioligand displacement assayBinding affinity to human ML1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2013.03.016
224 2440 133 None -1 9 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human ML1A receptor by radioligand displacement assayBinding affinity to human ML1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2013.03.016
896 2440 133 None -1 9 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human ML1A receptor by radioligand displacement assayBinding affinity to human ML1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2013.03.016
CHEMBL45 2440 133 None -1 9 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human ML1A receptor by radioligand displacement assayBinding affinity to human ML1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2013.03.016
DB01065 2440 133 None -1 9 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human ML1A receptor by radioligand displacement assayBinding affinity to human ML1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2013.03.016
23725612 125324 0 None -2 2 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 4 1 4 2.4 COc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 nan
CHEMBL3648367 125324 0 None -2 2 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 4 1 4 2.4 COc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 nan
10059864 109322 4 None 2 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL323332 109322 4 None 2 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
1357 2440 133 None -1 9 Human 9.2 pIC50 = 9.2 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/s0960-894x(03)00090-8
1672 2440 133 None -1 9 Human 9.2 pIC50 = 9.2 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/s0960-894x(03)00090-8
224 2440 133 None -1 9 Human 9.2 pIC50 = 9.2 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/s0960-894x(03)00090-8
896 2440 133 None -1 9 Human 9.2 pIC50 = 9.2 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/s0960-894x(03)00090-8
CHEMBL45 2440 133 None -1 9 Human 9.2 pIC50 = 9.2 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/s0960-894x(03)00090-8
DB01065 2440 133 None -1 9 Human 9.2 pIC50 = 9.2 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/s0960-894x(03)00090-8
57781246 125323 0 None -2 2 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 284 4 1 3 3.3 CC(=O)NCCC1CCc2ccc3nc(C4CC4)oc3c21 nan
CHEMBL3648366 125323 0 None -2 2 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 284 4 1 3 3.3 CC(=O)NCCC1CCc2ccc3nc(C4CC4)oc3c21 nan
44359126 28575 1 None - 0 Human 9.1 pIC50 = 9.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 6 1 2 3.3 CCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
CHEMBL137878 28575 1 None - 0 Human 9.1 pIC50 = 9.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 6 1 2 3.3 CCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
44359127 28714 1 None - 0 Human 9.1 pIC50 = 9.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 2 2.9 CCOc1ccc2cccc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL137998 28714 1 None - 0 Human 9.1 pIC50 = 9.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 2 2.9 CCOc1ccc2cccc(CCNC(C)=O)c2c1 10.1021/jm980026p
594980 109190 13 None - 0 Human 9.1 pIC50 = 9.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 286 4 2 2 2.4 COc1ccc2[nH]cc(CCNC(=O)C(F)(F)F)c2c1 10.1021/jm980026p
CHEMBL322762 109190 13 None - 0 Human 9.1 pIC50 = 9.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 286 4 2 2 2.4 COc1ccc2[nH]cc(CCNC(=O)C(F)(F)F)c2c1 10.1021/jm980026p
9859969 174441 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 259 4 1 2 3.2 CSc1ccc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
CHEMBL456727 174441 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 259 4 1 2 3.2 CSc1ccc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
57781227 125311 0 None -6 2 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 244 3 1 3 2.4 CC(=O)NCCC1CCc2ccc3ncoc3c21 nan
CHEMBL3648354 125311 0 None -6 2 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 244 3 1 3 2.4 CC(=O)NCCC1CCc2ccc3ncoc3c21 nan
1357 2440 133 None -1 9 Human 9.0 pIC50 = 9 Binding
Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980026p
1672 2440 133 None -1 9 Human 9.0 pIC50 = 9 Binding
Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980026p
224 2440 133 None -1 9 Human 9.0 pIC50 = 9 Binding
Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980026p
896 2440 133 None -1 9 Human 9.0 pIC50 = 9 Binding
Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980026p
CHEMBL45 2440 133 None -1 9 Human 9.0 pIC50 = 9 Binding
Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980026p
DB01065 2440 133 None -1 9 Human 9.0 pIC50 = 9 Binding
Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980026p
115348 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
1343 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
CHEMBL289233 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
DB08190 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
9834952 29092 0 None - 0 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 3 1 3 2.4 CC(=O)NCCc1coc2ccc3c(c12)CCCO3 10.1021/jm980026p
CHEMBL138321 29092 0 None - 0 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 3 1 3 2.4 CC(=O)NCCc1coc2ccc3c(c12)CCCO3 10.1021/jm980026p
10265261 141418 0 None - 0 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 272 2 1 3 2.7 COc1ccc2c(c1)c1c(n2C)CCCC1NC(C)=O 10.1021/jm980026p
CHEMBL38728 141418 0 None - 0 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 272 2 1 3 2.7 COc1ccc2c(c1)c1c(n2C)CCCC1NC(C)=O 10.1021/jm980026p
34247 8151 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 4 1 3 2.6 COc1ccc2scc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL109235 8151 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 4 1 3 2.6 COc1ccc2scc(CCNC(C)=O)c2c1 10.1021/jm980026p
9975634 9640 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 5 2 2 2.3 COc1ccc2[nH]cc(CCNC(=O)CI)c2c1 10.1021/jm980026p
CHEMBL113441 9640 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 5 2 2 2.3 COc1ccc2[nH]cc(CCNC(=O)CI)c2c1 10.1021/jm980026p
15340631 9734 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 253 3 1 2 3.3 CC(=O)NCCc1cccc2ccc3occc3c12 10.1021/jm980026p
CHEMBL11404 9734 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 253 3 1 2 3.3 CC(=O)NCCc1cccc2ccc3occc3c12 10.1021/jm980026p
164405 162189 9 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 5 1 2 2.9 COc1ccc2cccc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
CHEMBL417151 162189 9 None - 0 Human 8.9 pIC50 = 8.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 5 1 2 2.9 COc1ccc2cccc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
10059864 109322 4 None 2 2 Human 8.8 pIC50 = 8.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL323332 109322 4 None 2 2 Human 8.8 pIC50 = 8.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
10061999 7940 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 276 5 2 2 2.4 COc1cc2c(CCNC(=O)C3CC3)c[nH]c2cc1F 10.1021/jm980026p
CHEMBL109086 7940 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 276 5 2 2 2.4 COc1cc2c(CCNC(=O)C3CC3)c[nH]c2cc1F 10.1021/jm980026p
44358991 29622 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 283 7 1 2 3.5 C=CCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
CHEMBL138766 29622 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 283 7 1 2 3.5 C=CCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
3071631 138118 6 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 2 2.9 CCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL37771 138118 6 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 2 2.9 CCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
10038961 9617 0 None - 0 Human 8.0 pIC50 = 8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 3 1 2 3.0 CC(=O)NCCC1CCCc2ccc3c(c21)CCCO3 10.1021/jm980026p
CHEMBL11328 9617 0 None - 0 Human 8.0 pIC50 = 8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 3 1 2 3.0 CC(=O)NCCC1CCCc2ccc3c(c21)CCCO3 10.1021/jm980026p
9993398 29059 2 None - 0 Human 8.0 pIC50 = 8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 272 5 2 2 2.7 CCNC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL138288 29059 2 None - 0 Human 8.0 pIC50 = 8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 272 5 2 2 2.7 CCNC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
10131203 118222 1 None - 0 Human 8.0 pIC50 = 8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 4 1 3 2.2 CNC(=O)CCCc1cccc2c1SCCO2 10.1021/jm980026p
CHEMBL341761 118222 1 None - 0 Human 8.0 pIC50 = 8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 4 1 3 2.2 CNC(=O)CCCc1cccc2c1SCCO2 10.1021/jm980026p
4284525 188118 38 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL504585 188118 38 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
3071635 9298 3 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 4 0 2 3.0 COc1ccc2cccc(CCN3CCCC3=O)c2c1 10.1021/jm980026p
CHEMBL111558 9298 3 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 4 0 2 3.0 COc1ccc2cccc(CCN3CCCC3=O)c2c1 10.1021/jm980026p
21469690 28521 1 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 262 4 2 2 2.9 CCc1ccc2scc(CCNC(=O)NC)c2c1 10.1021/jm980026p
CHEMBL137823 28521 1 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 262 4 2 2 2.9 CCc1ccc2scc(CCNC(=O)NC)c2c1 10.1021/jm980026p
44359466 118638 0 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 283 6 1 4 1.9 CCS(=O)(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL342949 118638 0 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 283 6 1 4 1.9 CCS(=O)(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
4284525 188118 38 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
CHEMBL504585 188118 38 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
18177433 29167 0 None - 0 Human 6.0 pIC50 = 6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 4 1 3 1.8 COc1ccc2c(c1)CC(CCNC(C)=O)CO2 10.1021/jm980026p
CHEMBL138387 29167 0 None - 0 Human 6.0 pIC50 = 6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 4 1 3 1.8 COc1ccc2c(c1)CC(CCNC(C)=O)CO2 10.1021/jm980026p
44358869 118352 1 None - 0 Human 6.0 pIC50 = 6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 229 4 1 2 2.3 COc1ccc2cccc(CCC(N)=O)c2c1 10.1021/jm980026p
CHEMBL342207 118352 1 None - 0 Human 6.0 pIC50 = 6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 229 4 1 2 2.3 COc1ccc2cccc(CCC(N)=O)c2c1 10.1021/jm980026p
18357874 164485 2 None - 0 Human 6.0 pIC50 = 6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 219 3 1 3 1.8 CC(=O)NCCC1=COc2ccccc2O1 10.1021/jm980026p
CHEMBL422636 164485 2 None - 0 Human 6.0 pIC50 = 6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 219 3 1 3 1.8 CC(=O)NCCC1=COc2ccccc2O1 10.1021/jm980026p
19703067 28689 2 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 203 3 1 3 1.2 CC(=O)NCCn1ccc2cccnc21 10.1021/jm980026p
CHEMBL137970 28689 2 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 203 3 1 3 1.2 CC(=O)NCCn1ccc2cccnc21 10.1021/jm980026p
12288745 29075 2 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 221 2 1 3 1.1 COc1ccc2c(c1)CC(NC(C)=O)CO2 10.1021/jm980026p
CHEMBL138301 29075 2 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 221 2 1 3 1.1 COc1ccc2c(c1)CC(NC(C)=O)CO2 10.1021/jm980026p
19703053 29264 2 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 234 4 1 4 1.5 COc1nccc2c(CCNC(C)=O)coc12 10.1021/jm980026p
CHEMBL138468 29264 2 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 234 4 1 4 1.5 COc1nccc2c(CCNC(C)=O)coc12 10.1021/jm980026p
18175018 29309 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 260 4 2 2 2.2 CC(=O)NCCC1CCc2ccc(NC(C)=O)cc21 10.1021/jm980026p
CHEMBL138508 29309 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 260 4 2 2 2.2 CC(=O)NCCC1CCc2ccc(NC(C)=O)cc21 10.1021/jm980026p
15838838 30021 3 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 207 2 1 3 1.1 CC(=O)NCc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL139091 30021 3 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 207 2 1 3 1.1 CC(=O)NCc1cccc2c1OCCO2 10.1021/jm980026p
15372705 30404 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 4 1 4 3.0 COc1ccc2c(c1)OC(CNC(C)=O)=C(c1ccccc1)O2 10.1021/jm980026p
CHEMBL139418 30404 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 4 1 4 3.0 COc1ccc2c(c1)OC(CNC(C)=O)=C(c1ccccc1)O2 10.1021/jm980026p
15391788 31475 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 1 1 4 0.9 CC(=O)NC1COc2cc3c(cc2C1)OCCO3 10.1021/jm980026p
CHEMBL140548 31475 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 1 1 4 0.9 CC(=O)NC1COc2cc3c(cc2C1)OCCO3 10.1021/jm980026p
44359047 118733 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 3 1 4 0.5 CNC(=O)CCc1cccc2c1S(=O)(=O)CCO2 10.1021/jm980026p
CHEMBL343575 118733 0 None - 0 Human 5.0 pIC50 = 5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 3 1 4 0.5 CNC(=O)CCc1cccc2c1S(=O)(=O)CCO2 10.1021/jm980026p
15149134 99726 1 None - 0 Human 4.0 pIC50 = 4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 313 9 1 2 4.5 CCCCCCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL288300 99726 1 None - 0 Human 4.0 pIC50 = 4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 313 9 1 2 4.5 CCCCCCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
44359375 118703 3 None - 0 Human 4.0 pIC50 = 4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 211 1 1 1 2.4 O=C1CC(c2cccc3ccccc23)CN1 10.1021/jm980026p
CHEMBL343381 118703 3 None - 0 Human 4.0 pIC50 = 4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 211 1 1 1 2.4 O=C1CC(c2cccc3ccccc23)CN1 10.1021/jm980026p
23725566 125317 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 3.1 CCC(=O)NCC[C@H]1CCc2ccc3nc(C)oc3c21 nan
CHEMBL3648360 125317 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 272 4 1 3 3.1 CCC(=O)NCC[C@H]1CCc2ccc3nc(C)oc3c21 nan
44272486 69470 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 302 3 0 3 2.5 COc1ccc2c(c1)[C@H](N1CCN(C(=O)C(C)C)CC1)CC2 10.1016/s0960-894x(03)00090-8
CHEMBL19374 69470 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 302 3 0 3 2.5 COc1ccc2c(c1)[C@H](N1CCN(C(=O)C(C)C)CC1)CC2 10.1016/s0960-894x(03)00090-8
44358830 30179 2 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 5 1 4 1.5 COc1ccc2occ(CCNS(C)(=O)=O)c2c1 10.1021/jm980026p
CHEMBL139228 30179 2 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 5 1 4 1.5 COc1ccc2occ(CCNS(C)(=O)=O)c2c1 10.1021/jm980026p
44359427 30484 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 373 5 1 2 3.1 COc1ccc2c(c1)C(CCNC(=O)CI)CCC2 10.1021/jm980026p
CHEMBL139516 30484 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 373 5 1 2 3.1 COc1ccc2c(c1)C(CCNC(=O)CI)CCC2 10.1021/jm980026p
19696845 116020 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 243 4 1 2 2.5 CNC(=O)CCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL336225 116020 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 243 4 1 2 2.5 CNC(=O)CCc1cccc2ccc(OC)cc12 10.1021/jm980026p
44359390 118488 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 295 7 1 2 3.5 C=CCOc1ccc2cccc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
CHEMBL342592 118488 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 295 7 1 2 3.5 C=CCOc1ccc2cccc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
19385775 118911 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 274 4 2 2 2.9 CN/C(S)=N/CCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL344880 118911 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 274 4 2 2 2.9 CN/C(S)=N/CCc1cccc2ccc(OC)cc12 10.1021/jm980026p
44576404 192495 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 286 5 2 3 1.9 CNC(=O)c1ccc2occ(CCNC(=O)C3CC3)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL522674 192495 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 286 5 2 3 1.9 CNC(=O)c1ccc2occ(CCNC(=O)C3CC3)c2c1 10.1016/j.bmc.2008.03.036
10399169 28663 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 235 4 1 3 1.5 CC(=O)NCCCc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL137948 28663 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 235 4 1 3 1.5 CC(=O)NCCCc1cccc2c1OCCO2 10.1021/jm980026p
19703063 28687 1 None 2 2 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1021/jm980026p
CHEMBL137969 28687 1 None 2 2 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1021/jm980026p
23360853 31818 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 6 1 3 3.1 COc1ccc2cc(C(C)=O)cc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
CHEMBL140826 31818 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 6 1 3 3.1 COc1ccc2cc(C(C)=O)cc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
44359206 118860 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 265 5 1 3 2.6 CC(=O)NCCCCc1cccc2c1SCCO2 10.1021/jm980026p
CHEMBL344488 118860 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 265 5 1 3 2.6 CC(=O)NCCCCc1cccc2c1SCCO2 10.1021/jm980026p
44359079 164693 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 247 5 1 3 2.5 CCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL423011 164693 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 247 5 1 3 2.5 CCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
44358887 26641 1 None - 0 Human 5.9 pIC50 = 5.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 215 2 1 2 2.2 CNC(=O)c1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL136346 26641 1 None - 0 Human 5.9 pIC50 = 5.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 215 2 1 2 2.2 CNC(=O)c1cccc2ccc(OC)cc12 10.1021/jm980026p
44359058 29451 3 None - 0 Human 4.9 pIC50 = 4.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 203 3 2 2 1.2 CC(=O)NCCc1c[nH]c2ncccc12 10.1021/jm980026p
CHEMBL138631 29451 3 None - 0 Human 4.9 pIC50 = 4.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 203 3 2 2 1.2 CC(=O)NCCc1c[nH]c2ncccc12 10.1021/jm980026p
23725513 125314 0 None -3 2 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@H]1CCc2ccc3nc(C)oc3c21 nan
CHEMBL3648357 125314 0 None -3 2 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@H]1CCc2ccc3nc(C)oc3c21 nan
15340629 9758 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 3 1 3 2.1 CC(=O)NCCc1cccc2ccc3c(c12)C(=O)CO3 10.1021/jm980026p
CHEMBL11416 9758 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 3 1 3 2.1 CC(=O)NCCc1cccc2ccc3c(c12)C(=O)CO3 10.1021/jm980026p
44359205 28703 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 299 8 1 2 4.1 CCCCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
CHEMBL137983 28703 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 299 8 1 2 4.1 CCCCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
44358971 28761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 3 2.1 C#CCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL138037 28761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 3 2.1 C#CCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
10059969 28783 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 235 4 1 3 1.5 CNC(=O)CCCc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL138053 28783 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 235 4 1 3 1.5 CNC(=O)CCCc1cccc2c1OCCO2 10.1021/jm980026p
15289277 28962 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 333 6 1 2 4.1 COc1ccc2cc(Cc3ccccc3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL138201 28962 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 333 6 1 2 4.1 COc1ccc2cc(Cc3ccccc3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
23360848 161110 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 6 1 2 3.5 CCc1cc(CCNC(=O)C2CC2)c2cc(OC)ccc2c1 10.1021/jm980026p
CHEMBL413121 161110 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 6 1 2 3.5 CCc1cc(CCNC(=O)C2CC2)c2cc(OC)ccc2c1 10.1021/jm980026p
22375366 69135 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 300 3 0 3 2.2 COc1ccc2c(c1)C(N1CCN(C(=O)C3CC3)CC1)CC2 10.1016/s0960-894x(03)00090-8
CHEMBL19339 69135 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 300 3 0 3 2.2 COc1ccc2c(c1)C(N1CCN(C(=O)C3CC3)CC1)CC2 10.1016/s0960-894x(03)00090-8
44358744 26488 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 5 1 3 1.9 CC(=O)NCCCCc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL136214 26488 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 5 1 3 1.9 CC(=O)NCCCCc1cccc2c1OCCO2 10.1021/jm980026p
15340628 27195 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 287 6 2 3 2.0 CC(=O)NCCc1cccc2ccc(OCC(=O)O)cc12 10.1021/jm980026p
CHEMBL136815 27195 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 287 6 2 3 2.0 CC(=O)NCCc1cccc2ccc(OCC(=O)O)cc12 10.1021/jm980026p
10060719 169857 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 4 1 3 2.2 CC(=O)NCCCc1cccc2c1SCCO2 10.1021/jm980026p
CHEMBL444857 169857 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 4 1 3 2.2 CC(=O)NCCCc1cccc2c1SCCO2 10.1021/jm980026p
44359046 29633 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 265 6 1 4 1.8 CC(=O)NCCCCOc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL138774 29633 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 265 6 1 4 1.8 CC(=O)NCCCCOc1cccc2c1OCCO2 10.1021/jm980026p
18782997 32967 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 277 6 2 4 1.6 CC(=O)NCCc1coc2ccc(OCC(=O)O)cc12 10.1021/jm980026p
CHEMBL141785 32967 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 277 6 2 4 1.6 CC(=O)NCCc1coc2ccc(OCC(=O)O)cc12 10.1021/jm980026p
19703028 118625 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 204 3 1 3 1.5 CC(=O)NCCc1coc2cnccc12 10.1021/jm980026p
CHEMBL342836 118625 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 204 3 1 3 1.5 CC(=O)NCCc1coc2cnccc12 10.1021/jm980026p
44359374 118882 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 241 2 1 2 2.5 COc1ccc2cccc(C3CNC(=O)C3)c2c1 10.1021/jm980026p
CHEMBL344632 118882 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 241 2 1 2 2.5 COc1ccc2cccc(C3CNC(=O)C3)c2c1 10.1021/jm980026p
21460931 167879 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 245 5 1 2 3.1 CCCc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL435032 167879 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 245 5 1 2 3.1 CCCc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
15391785 28936 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 3 1 3 1.6 COc1ccc2c(c1)C=C(CNC(C)=O)CO2 10.1021/jm980026p
CHEMBL138180 28936 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 3 1 3 1.6 COc1ccc2c(c1)C=C(CNC(C)=O)CO2 10.1021/jm980026p
44358928 29939 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 333 7 1 2 4.1 COc1ccc2cccc(CC(=O)NCCCc3ccccc3)c2c1 10.1021/jm980026p
CHEMBL139016 29939 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 333 7 1 2 4.1 COc1ccc2cccc(CC(=O)NCCCc3ccccc3)c2c1 10.1021/jm980026p
44359070 32564 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 205 3 1 3 0.6 CC(=O)NCCN1CCc2cccnc21 10.1021/jm980026p
CHEMBL141430 32564 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 205 3 1 3 0.6 CC(=O)NCCN1CCc2cccnc21 10.1021/jm980026p
22375372 66907 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 302 3 0 3 2.5 COc1ccc2c(c1)C(N1CCN(C(=O)C(C)C)CC1)CC2 10.1016/s0960-894x(03)00090-8
CHEMBL18808 66907 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 302 3 0 3 2.5 COc1ccc2c(c1)C(N1CCN(C(=O)C(C)C)CC1)CC2 10.1016/s0960-894x(03)00090-8
11059058 9981 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against melatonin receptor type 1ABinding affinity against melatonin receptor type 1A
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
CHEMBL115444 9981 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against melatonin receptor type 1ABinding affinity against melatonin receptor type 1A
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
44576399 188190 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 260 4 2 3 1.5 CNC(=O)c1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL505744 188190 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 260 4 2 3 1.5 CNC(=O)c1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
23725568 125321 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 3 1 3 3.2 CC(=O)NCC[C@H]1CCc2ccc3nc(C)sc3c21 nan
CHEMBL3648364 125321 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2.
ChEMBL 274 3 1 3 3.2 CC(=O)NCC[C@H]1CCc2ccc3nc(C)sc3c21 nan
10039072 28664 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 6 3 2 2.4 CCCNC(=O)NCCc1c[nH]c2ccc(OC)cc12 10.1021/jm980026p
CHEMBL137949 28664 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 6 3 2 2.4 CCCNC(=O)NCCc1c[nH]c2ccc(OC)cc12 10.1021/jm980026p
10377971 29297 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 5 1 3 2.4 CCCC(=O)NCC1=Cc2cc(OC)ccc2OC1 10.1021/jm980026p
CHEMBL138496 29297 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 5 1 3 2.4 CCCC(=O)NCC1=Cc2cc(OC)ccc2OC1 10.1021/jm980026p
44359437 29671 0 None 1 3 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 5 2 3 2.1 COc1ccc2cccc(C(CO)CNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL138807 29671 0 None 1 3 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 5 2 3 2.1 COc1ccc2cccc(C(CO)CNC(C)=O)c2c1 10.1021/jm980026p
19752678 29673 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 243 5 1 2 2.7 COc1ccc2cccc(CCCC(N)=O)c2c1 10.1021/jm980026p
CHEMBL138808 29673 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 243 5 1 2 2.7 COc1ccc2cccc(CCCC(N)=O)c2c1 10.1021/jm980026p
10448305 29830 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 313 9 1 2 4.5 CCCCCCOc1ccc2cccc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL138924 29830 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 313 9 1 2 4.5 CCCCCCOc1ccc2cccc(CCNC(C)=O)c2c1 10.1021/jm980026p
44359018 118926 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 5 1 3 2.5 COc1ccc2occ(CCNC(=O)CBr)c2c1 10.1021/jm980026p
CHEMBL345029 118926 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 5 1 3 2.5 COc1ccc2occ(CCNC(=O)CBr)c2c1 10.1021/jm980026p
44358910 27196 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 7 1 2 3.7 CCCOc1ccc2cccc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
CHEMBL136816 27196 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 7 1 2 3.7 CCCOc1ccc2cccc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
2821758 29129 15 None - 0 Human 5.7 pIC50 = 5.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 207 2 1 3 1.0 CC(=O)NCC1COc2ccccc2O1 10.1021/jm980026p
CHEMBL138355 29129 15 None - 0 Human 5.7 pIC50 = 5.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 207 2 1 3 1.0 CC(=O)NCC1COc2ccccc2O1 10.1021/jm980026p
44358944 32668 3 None - 0 Human 5.7 pIC50 = 5.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 286 9 2 1 4.2 CCCCCCCC(=O)NCCc1c[nH]c2ccccc12 10.1021/jm980026p
CHEMBL141522 32668 3 None - 0 Human 5.7 pIC50 = 5.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 286 9 2 1 4.2 CCCCCCCC(=O)NCCc1c[nH]c2ccccc12 10.1021/jm980026p
15149133 119497 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 299 8 1 2 4.1 CCCCCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL35017 119497 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 299 8 1 2 4.1 CCCCCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
53827707 110364 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK293 cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 279 6 1 3 3.0 CCCNC(=O)CCCc1cccc2c1SCCO2 10.1021/jm401343c
CHEMBL3260981 110364 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK293 cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 279 6 1 3 3.0 CCCNC(=O)CCCc1cccc2c1SCCO2 10.1021/jm401343c
18360745 29685 1 None - 0 Human 8.6 pIC50 = 8.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 258 4 2 2 2.3 CNC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL138817 29685 1 None - 0 Human 8.6 pIC50 = 8.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 258 4 2 2 2.3 CNC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
3071630 137698 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 5 1 2 3.2 COc1ccc2cccc(CCNC(=O)C(C)C)c2c1 10.1021/jm980026p
CHEMBL37703 137698 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 5 1 2 3.2 COc1ccc2cccc(CCNC(=O)C(C)C)c2c1 10.1021/jm980026p
10266979 98549 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 303 3 1 3 2.0 CCNC(=O)N1CCN([C@@H]2CCc3ccc(OC)cc32)CC1 10.1016/s0960-894x(03)00090-8
CHEMBL280142 98549 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 303 3 1 3 2.0 CCNC(=O)N1CCN([C@@H]2CCc3ccc(OC)cc32)CC1 10.1016/s0960-894x(03)00090-8
11178762 66656 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 463 5 0 2 6.1 COc1cc2c(cc1Br)CCN(C(C)=O)C2CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.09.024
CHEMBL186941 66656 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 463 5 0 2 6.1 COc1cc2c(cc1Br)CCN(C(C)=O)C2CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.09.024
44340895 9314 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 219 3 1 2 1.9 COc1ccc2c(c1)C(CNC(C)=O)CC2 10.1021/jm980026p
CHEMBL111667 9314 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 219 3 1 2 1.9 COc1ccc2c(c1)C(CNC(C)=O)CC2 10.1021/jm980026p
44359479 29944 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 277 6 1 3 3.4 CCCOc1ccc2scc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL139021 29944 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 277 6 1 3 3.4 CCCOc1ccc2scc(CCNC(C)=O)c2c1 10.1021/jm980026p
44359019 31368 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 6 1 3 2.7 C=CCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL140427 31368 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 6 1 3 2.7 C=CCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
19086015 30413 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 300 7 2 2 3.5 CCCNC(=O)NCCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL139428 30413 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 300 7 2 2 3.5 CCCNC(=O)NCCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
19703043 118808 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 5 1 4 1.7 COc1cnc2c(c1)c(CCNC(=O)C1CC1)cn2C 10.1021/jm980026p
CHEMBL344179 118808 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 5 1 4 1.7 COc1cnc2c(c1)c(CCNC(=O)C1CC1)cn2C 10.1021/jm980026p
3071647 135808 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 344 5 2 2 4.3 COc1ccc2cccc(CCNC(=O)c3cc4ccccc4[nH]3)c2c1 10.1021/jm980026p
CHEMBL37341 135808 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 344 5 2 2 4.3 COc1ccc2cccc(CCNC(=O)c3cc4ccccc4[nH]3)c2c1 10.1021/jm980026p
18175032 175013 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 358 6 2 4 2.3 CNS(=O)(=O)c1ccc2cccc(CCNC(=O)c3ccco3)c2c1 10.1016/j.ejmech.2011.02.010
CHEMBL457992 175013 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 358 6 2 4 2.3 CNS(=O)(=O)c1ccc2cccc(CCNC(=O)c3ccco3)c2c1 10.1016/j.ejmech.2011.02.010
44593610 186779 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 302 6 2 4 2.8 C=CCC(=O)NCCc1coc2ccc(NC(=O)OC)cc12 10.1016/j.bmc.2008.03.036
CHEMBL493424 186779 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 302 6 2 4 2.8 C=CCC(=O)NCCc1coc2ccc(NC(=O)OC)cc12 10.1016/j.bmc.2008.03.036
44359035 31477 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 285 7 1 2 3.7 CCCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
CHEMBL140549 31477 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 285 7 1 2 3.7 CCCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
18947294 32176 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 248 4 2 3 1.9 CNC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL141115 32176 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 248 4 2 3 1.9 CNC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
44359270 168030 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 283 6 2 2 3.3 C=CCc1c(O)ccc2cccc(CCNC(=O)CC)c12 10.1021/jm980026p
CHEMBL436006 168030 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 283 6 2 2 3.3 C=CCc1c(O)ccc2cccc(CCNC(=O)CC)c12 10.1021/jm980026p
10333620 108704 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 5 1 3 3.0 COc1ccc2scc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
CHEMBL321612 108704 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 5 1 3 3.0 COc1ccc2scc(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
44359308 114978 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 244 4 2 2 2.1 COc1ccc2cccc(CCNC(N)=O)c2c1 10.1021/jm980026p
CHEMBL335116 114978 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 244 4 2 2 2.1 COc1ccc2cccc(CCNC(N)=O)c2c1 10.1021/jm980026p
18783022 116243 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 3 1 3 2.5 CC(=O)NCCc1coc2ccc3c(c12)C=CCO3 10.1021/jm980026p
CHEMBL337580 116243 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 3 1 3 2.5 CC(=O)NCCc1coc2ccc3c(c12)C=CCO3 10.1021/jm980026p
19967248 168742 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 6 1 3 3.2 CCCC(=O)NOCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL441664 168742 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 273 6 1 3 3.2 CCCC(=O)NOCc1cccc2ccc(OC)cc12 10.1021/jm980026p
18175008 174912 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 292 4 2 3 1.2 CC(=O)NCCc1cccc2ccc(S(N)(=O)=O)cc12 10.1016/j.ejmech.2011.02.010
CHEMBL457763 174912 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 292 4 2 3 1.2 CC(=O)NCCc1cccc2ccc(S(N)(=O)=O)cc12 10.1016/j.ejmech.2011.02.010
44358896 30479 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 228 3 2 1 2.3 CNC(=O)NCCc1cccc2ccccc12 10.1021/jm980026p
CHEMBL139510 30479 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 228 3 2 1 2.3 CNC(=O)NCCc1cccc2ccccc12 10.1021/jm980026p
44358943 31166 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 5 1 2 4.2 CC(=O)NCCc1cccc2ccc(OC3CCCCC3)cc12 10.1021/jm980026p
CHEMBL140244 31166 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 5 1 2 4.2 CC(=O)NCCc1cccc2ccc(OC3CCCCC3)cc12 10.1021/jm980026p
10243074 9690 2 None - 0 Human 5.5 pIC50 = 5.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 1 4 1.2 COc1ccc2ncn(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL113692 9690 2 None - 0 Human 5.5 pIC50 = 5.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 1 4 1.2 COc1ccc2ncn(CCNC(C)=O)c2c1 10.1021/jm980026p
44359228 30074 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 237 4 1 4 1.0 CC(=O)NCCOc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL139133 30074 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 237 4 1 4 1.0 CC(=O)NCCOc1cccc2c1OCCO2 10.1021/jm980026p
15372706 118909 1 None - 0 Human 4.5 pIC50 = 4.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 281 3 1 3 3.0 CC(=O)NCC1=C(c2ccccc2)Oc2ccccc2O1 10.1021/jm980026p
CHEMBL344866 118909 1 None - 0 Human 4.5 pIC50 = 4.5 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 281 3 1 3 3.0 CC(=O)NCC1=C(c2ccccc2)Oc2ccccc2O1 10.1021/jm980026p
9861677 186966 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 315 5 1 4 3.1 COC(=O)c1ccc2occ(CCNC(=O)C3CCCC3)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL494566 186966 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 315 5 1 4 3.1 COC(=O)c1ccc2occ(CCNC(=O)C3CCCC3)c2c1 10.1016/j.bmc.2008.03.036
10379422 8337 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 289 5 1 3 3.4 COc1ccc2scc(CCNC(=O)C3CCC3)c2c1 10.1021/jm980026p
CHEMBL109361 8337 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 289 5 1 3 3.4 COc1ccc2scc(CCNC(=O)C3CCC3)c2c1 10.1021/jm980026p
15391789 29385 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 235 3 1 3 1.4 COc1ccc2c(c1)CC(CNC(C)=O)CO2 10.1021/jm980026p
CHEMBL138581 29385 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 235 3 1 3 1.4 COc1ccc2c(c1)CC(CNC(C)=O)CO2 10.1021/jm980026p
23360817 30561 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 6 1 3 3.1 COc1ccc2cc(C(=O)C3CC3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL139627 30561 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 311 6 1 3 3.1 COc1ccc2cc(C(=O)C3CC3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
44359020 31374 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 337 7 1 3 4.1 CCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL140433 31374 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 337 7 1 3 4.1 CCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm980026p
44358768 116281 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 6 1 3 2.8 CCCC(=O)NCCCc1cccc2c1OC=CO2 10.1021/jm980026p
CHEMBL337802 116281 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 6 1 3 2.8 CCCC(=O)NCCCc1cccc2c1OC=CO2 10.1021/jm980026p
44358840 118229 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 4 1 3 2.7 COC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL341802 118229 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 4 1 3 2.7 COC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
2368416 99606 5 None - 0 Human 5.4 pIC50 = 5.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 242 4 2 1 2.6 O=C(NCCc1c[nH]c2ccccc12)C1CCC1 10.1021/jm980026p
CHEMBL287310 99606 5 None - 0 Human 5.4 pIC50 = 5.4 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 242 4 2 1 2.6 O=C(NCCc1c[nH]c2ccccc12)C1CCC1 10.1021/jm980026p
44272591 71346 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 300 3 0 3 2.2 COc1ccc2c(c1)[C@H](N1CCN(C(=O)C3CC3)CC1)CC2 10.1016/s0960-894x(03)00090-8
CHEMBL19653 71346 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro receptor binding at MT1 (Melatonin) receptor.In vitro receptor binding at MT1 (Melatonin) receptor.
ChEMBL 300 3 0 3 2.2 COc1ccc2c(c1)[C@H](N1CCN(C(=O)C3CC3)CC1)CC2 10.1016/s0960-894x(03)00090-8
21916760 175116 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 291 4 1 3 1.9 CC(=O)NCCc1cccc2ccc(S(C)(=O)=O)cc12 10.1016/j.ejmech.2011.02.010
CHEMBL458209 175116 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 291 4 1 3 1.9 CC(=O)NCCc1cccc2ccc(S(C)(=O)=O)cc12 10.1016/j.ejmech.2011.02.010
10422677 9199 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 5 1 3 2.5 COc1ccc2occ(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
CHEMBL110980 9199 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 5 1 3 2.5 COc1ccc2occ(CCNC(=O)C3CC3)c2c1 10.1021/jm980026p
18783019 28612 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 267 5 1 2 2.5 C#CCOc1ccc2cccc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL137910 28612 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 267 5 1 2 2.5 C#CCOc1ccc2cccc(CCNC(C)=O)c2c1 10.1021/jm980026p
44359309 29229 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 4 2 3 2.0 COc1ccc2cccc(C(O)CNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL138440 29229 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 4 2 3 2.0 COc1ccc2cccc(C(O)CNC(C)=O)c2c1 10.1021/jm980026p
9881916 29607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 2 1 3 2.3 COc1ccc2ccc3c(c2c1)CC(NC(C)=O)CO3 10.1021/jm980026p
CHEMBL138752 29607 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 2 1 3 2.3 COc1ccc2ccc3c(c2c1)CC(NC(C)=O)CO3 10.1021/jm980026p
10248871 108065 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 375 5 1 3 3.0 COc1ccc2scc(CCNC(=O)CI)c2c1 10.1021/jm980026p
CHEMBL320253 108065 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 375 5 1 3 3.0 COc1ccc2scc(CCNC(=O)CI)c2c1 10.1021/jm980026p
44359464 29719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 7 1 3 3.3 CCCCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL138841 29719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 7 1 3 3.3 CCCCOc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
18947318 118280 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 293 6 3 2 2.6 CCCNC(=O)NCCc1c[nH]c2cc(F)c(OC)cc12 10.1021/jm980026p
CHEMBL342162 118280 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 293 6 3 2 2.6 CCCNC(=O)NCCc1c[nH]c2cc(F)c(OC)cc12 10.1021/jm980026p
44358743 118524 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 5 1 3 1.9 CNC(=O)CCCCc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL342649 118524 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 249 5 1 3 1.9 CNC(=O)CCCCc1cccc2c1OCCO2 10.1021/jm980026p
23360832 118765 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 299 6 1 3 3.1 CCC(=O)c1cc(CCNC(C)=O)c2cc(OC)ccc2c1 10.1021/jm980026p
CHEMBL343819 118765 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 299 6 1 3 3.1 CCC(=O)c1cc(CCNC(C)=O)c2cc(OC)ccc2c1 10.1021/jm980026p
22133298 118855 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 286 6 2 2 3.1 CCCNC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL344454 118855 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 286 6 2 2 3.1 CCCNC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
18175028 59749 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 306 5 2 3 1.4 CNS(=O)(=O)c1ccc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
CHEMBL1738752 59749 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 306 5 2 3 1.4 CNS(=O)(=O)c1ccc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
10085672 29278 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 291 7 1 3 3.8 CCCCC(=O)NCCc1csc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL138475 29278 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 291 7 1 3 3.8 CCCCC(=O)NCCc1csc2ccc(OC)cc12 10.1021/jm980026p
21572387 29512 3 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 214 3 2 1 2.1 NC(=O)NCCc1cccc2ccccc12 10.1021/jm980026p
CHEMBL138675 29512 3 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 214 3 2 1 2.1 NC(=O)NCCc1cccc2ccccc12 10.1021/jm980026p
44359120 29847 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 4 1 2 3.4 O=C(NCCc1csc2ccccc12)C1CCC1 10.1021/jm980026p
CHEMBL138938 29847 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 259 4 1 2 3.4 O=C(NCCc1csc2ccccc12)C1CCC1 10.1021/jm980026p
9837777 31906 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 247 4 1 4 1.3 COc1cnc2c(c1)c(CCNC(C)=O)cn2C 10.1021/jm980026p
CHEMBL140896 31906 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 247 4 1 4 1.3 COc1cnc2c(c1)c(CCNC(C)=O)cn2C 10.1021/jm980026p
15838839 32985 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 221 3 1 3 1.1 CC(=O)NCCc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL141796 32985 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 221 3 1 3 1.1 CC(=O)NCCc1cccc2c1OCCO2 10.1021/jm980026p
11749479 66549 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 385 5 0 2 5.4 COc1ccc2c(c1)C(CC(c1ccccc1)c1ccccc1)N(C(C)=O)CC2 10.1016/j.bmcl.2004.09.024
CHEMBL186452 66549 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 385 5 0 2 5.4 COc1ccc2c(c1)C(CC(c1ccccc1)c1ccccc1)N(C(C)=O)CC2 10.1016/j.bmcl.2004.09.024
44576406 186777 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 330 5 2 4 3.5 COC(=O)Nc1ccc2occ(CCNC(=O)C3CCCC3)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL493414 186777 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 330 5 2 4 3.5 COC(=O)Nc1ccc2occ(CCNC(=O)C3CCCC3)c2c1 10.1016/j.bmc.2008.03.036
17957007 192044 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 304 5 2 4 2.9 COC(=O)Nc1ccc2occ(CCNC(=O)C(C)C)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL521826 192044 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 304 5 2 4 2.9 COC(=O)Nc1ccc2occ(CCNC(=O)C(C)C)c2c1 10.1016/j.bmc.2008.03.036
10265421 9327 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 7 1 3 3.3 CCCCC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL111718 9327 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 275 7 1 3 3.3 CCCCC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
44359121 29936 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 313 9 1 2 4.5 CCCCCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
CHEMBL139014 29936 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 313 9 1 2 4.5 CCCCCOc1ccc2cccc(CCNC(=O)CC)c2c1 10.1021/jm980026p
23360808 30396 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 285 6 1 2 3.5 CCCc1cc(CCNC(C)=O)c2cc(OC)ccc2c1 10.1021/jm980026p
CHEMBL139410 30396 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 285 6 1 2 3.5 CCCc1cc(CCNC(C)=O)c2cc(OC)ccc2c1 10.1021/jm980026p
11361621 125273 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 401 7 0 3 5.0 COc1cc2c(cc1OC)C(CC(c1ccccc1)c1ccccc1)N(C=O)CC2 10.1016/j.bmcl.2004.09.024
CHEMBL364816 125273 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 401 7 0 3 5.0 COc1cc2c(cc1OC)C(CC(c1ccccc1)c1ccccc1)N(C=O)CC2 10.1016/j.bmcl.2004.09.024
18177435 28939 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 285 3 1 3 2.5 COc1ccc2ccc3c(c2c1)CC(CNC(C)=O)CO3 10.1021/jm980026p
CHEMBL138182 28939 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 285 3 1 3 2.5 COc1ccc2ccc3c(c2c1)CC(CNC(C)=O)CO3 10.1021/jm980026p
21469691 118628 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 5 1 2 3.5 CCC(=O)NCCc1csc2ccc(CC)cc12 10.1021/jm980026p
CHEMBL342855 118628 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 5 1 2 3.5 CCC(=O)NCCc1csc2ccc(CC)cc12 10.1021/jm980026p
21469682 31544 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 289 7 1 2 4.3 CCCCC(=O)NCCc1csc2ccc(CC)cc12 10.1021/jm980026p
CHEMBL140611 31544 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 289 7 1 2 4.3 CCCCC(=O)NCCc1csc2ccc(CC)cc12 10.1021/jm980026p
44359381 32287 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 5 1 4 1.4 CC(=O)NCCCOc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL141208 32287 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 5 1 4 1.4 CC(=O)NCCCOc1cccc2c1OCCO2 10.1021/jm980026p
44359294 116275 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 406 8 4 3 3.8 COc1ccc2[nH]cc(CCNC(=O)NCCc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/jm980026p
CHEMBL337767 116275 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 406 8 4 3 3.8 COc1ccc2[nH]cc(CCNC(=O)NCCc3c[nH]c4ccc(OC)cc34)c2c1 10.1021/jm980026p
17524911 31828 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 256 4 2 1 3.0 O=C(NCCc1c[nH]c2ccccc12)C1CCCC1 10.1021/jm980026p
CHEMBL140835 31828 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 256 4 2 1 3.0 O=C(NCCc1c[nH]c2ccccc12)C1CCCC1 10.1021/jm980026p
588712 32862 10 None - 0 Human 5.2 pIC50 = 5.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 244 6 2 1 3.0 CCCCC(=O)NCCc1c[nH]c2ccccc12 10.1021/jm980026p
CHEMBL141694 32862 10 None - 0 Human 5.2 pIC50 = 5.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 244 6 2 1 3.0 CCCCC(=O)NCCc1c[nH]c2ccccc12 10.1021/jm980026p
11430378 167645 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 431 6 0 4 5.6 COC(=O)N1CCc2cc(OC)c(OC)cc2C1CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.09.024
CHEMBL433573 167645 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against Melatonin receptor type 1AInhibitory concentration against Melatonin receptor type 1A
ChEMBL 431 6 0 4 5.6 COC(=O)N1CCc2cc(OC)c(OC)cc2C1CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.09.024
9837740 29354 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 245 4 1 3 2.4 COc1ccc2cccc(CONC(C)=O)c2c1 10.1021/jm980026p
CHEMBL138549 29354 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 245 4 1 3 2.4 COc1ccc2cccc(CONC(C)=O)c2c1 10.1021/jm980026p
44359113 115889 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 7 1 2 3.7 CCC(=O)NCCc1cccc2ccc(OCC3CC3)cc12 10.1021/jm980026p
CHEMBL336010 115889 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 7 1 2 3.7 CCC(=O)NCCc1cccc2ccc(OCC3CC3)cc12 10.1021/jm980026p
23360842 118459 1 None - 1 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 6 1 2 3.5 COc1ccc2cc(CC3CC3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL342432 118459 1 None - 1 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 6 1 2 3.5 COc1ccc2cc(CC3CC3)cc(CCNC(C)=O)c2c1 10.1021/jm980026p
44358970 118525 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 359 5 1 3 2.5 COc1ccc2occ(CCNC(=O)CI)c2c1 10.1021/jm980026p
CHEMBL342655 118525 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 359 5 1 3 2.5 COc1ccc2occ(CCNC(=O)CI)c2c1 10.1021/jm980026p
18947325 118825 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 262 5 2 3 2.3 CCNC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL344268 118825 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 262 5 2 3 2.3 CCNC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
9817006 174402 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 275 4 1 2 2.3 CC(=O)NCCc1cccc2ccc([S+](C)[O-])cc12 10.1016/j.ejmech.2011.02.010
CHEMBL456646 174402 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 275 4 1 2 2.3 CC(=O)NCCc1cccc2ccc([S+](C)[O-])cc12 10.1016/j.ejmech.2011.02.010
44358879 29837 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 6 1 2 3.7 CCOc1ccc2cccc(CCNC(=O)C3CCC3)c2c1 10.1021/jm980026p
CHEMBL138929 29837 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 297 6 1 2 3.7 CCOc1ccc2cccc(CCNC(=O)C3CCC3)c2c1 10.1021/jm980026p
44359266 31478 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 316 4 0 5 2.2 COc1ccc2c(c1)c(CCN(C(C)=O)C(C)=O)cn2C(C)=O 10.1021/jm980026p
CHEMBL140551 31478 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 316 4 0 5 2.2 COc1ccc2c(c1)c(CCN(C(C)=O)C(C)=O)cn2C(C)=O 10.1021/jm980026p
18947270 32654 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 276 6 2 3 2.7 CCCNC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL141507 32654 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 276 6 2 3 2.7 CCCNC(=O)NCCc1coc2ccc(OC)cc12 10.1021/jm980026p
44359465 118260 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 5 1 3 2.9 CC(=O)NCCc1coc2ccc(OC(C)C)cc12 10.1021/jm980026p
CHEMBL341989 118260 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 261 5 1 3 2.9 CC(=O)NCCc1coc2ccc(OC(C)C)cc12 10.1021/jm980026p
21469693 30649 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 290 6 2 2 3.7 CCCNC(=O)NCCc1csc2ccc(CC)cc12 10.1021/jm980026p
CHEMBL139744 30649 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 290 6 2 2 3.7 CCCNC(=O)NCCc1csc2ccc(CC)cc12 10.1021/jm980026p
18177465 118822 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 4 1 4 1.4 COc1ccc2c(c1)OC(CCNC(C)=O)CO2 10.1021/jm980026p
CHEMBL344242 118822 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 251 4 1 4 1.4 COc1ccc2c(c1)OC(CCNC(C)=O)CO2 10.1021/jm980026p
15838841 30016 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 280 6 2 4 1.5 CCCNC(=O)NCCOc1cccc2c1OCCO2 10.1021/jm980026p
CHEMBL139087 30016 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 280 6 2 4 1.5 CCCNC(=O)NCCOc1cccc2c1OCCO2 10.1021/jm980026p
25014882 187102 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 302 5 2 4 2.7 COC(=O)Nc1ccc2occ(CCNC(=O)C3CC3)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL495232 187102 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 302 5 2 4 2.7 COC(=O)Nc1ccc2occ(CCNC(=O)C3CC3)c2c1 10.1016/j.bmc.2008.03.036
17957000 61061 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 286 4 2 3 2.7 COC(=O)Nc1ccc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
CHEMBL1770214 61061 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 286 4 2 3 2.7 COC(=O)Nc1ccc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
1357 2440 133 None -1 9 Human 9.8 pKd = 9.8 Binding
Binding affinity to melatonin receptor MT1 (unknown origin)Binding affinity to melatonin receptor MT1 (unknown origin)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
1672 2440 133 None -1 9 Human 9.8 pKd = 9.8 Binding
Binding affinity to melatonin receptor MT1 (unknown origin)Binding affinity to melatonin receptor MT1 (unknown origin)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
224 2440 133 None -1 9 Human 9.8 pKd = 9.8 Binding
Binding affinity to melatonin receptor MT1 (unknown origin)Binding affinity to melatonin receptor MT1 (unknown origin)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
896 2440 133 None -1 9 Human 9.8 pKd = 9.8 Binding
Binding affinity to melatonin receptor MT1 (unknown origin)Binding affinity to melatonin receptor MT1 (unknown origin)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
CHEMBL45 2440 133 None -1 9 Human 9.8 pKd = 9.8 Binding
Binding affinity to melatonin receptor MT1 (unknown origin)Binding affinity to melatonin receptor MT1 (unknown origin)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
DB01065 2440 133 None -1 9 Human 9.8 pKd = 9.8 Binding
Binding affinity to melatonin receptor MT1 (unknown origin)Binding affinity to melatonin receptor MT1 (unknown origin)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
10440 2632 15 None -21 3 Human 5.2 pKd = 5.2 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2632 15 None -21 3 Human 5.2 pKd = 5.2 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2632 15 None -21 3 Human 5.2 pKd = 5.2 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
22004862 61678 0 None -1 2 Human 11.1 pKi = 11.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 319 4 1 2 3.6 CC(=O)NCCC1=C(c2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200385u
CHEMBL1774522 61678 0 None -1 2 Human 11.1 pKi = 11.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 319 4 1 2 3.6 CC(=O)NCCC1=C(c2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200385u
9903515 22576 0 None 9 2 Human 11.0 pKi = 11 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 3 1 2 3.0 COc1ccc2cccc3c2c1C(CNC(C)=O)CC3 10.1021/jm000922c
CHEMBL132802 22576 0 None 9 2 Human 11.0 pKi = 11 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 3 1 2 3.0 COc1ccc2cccc3c2c1C(CNC(C)=O)CC3 10.1021/jm000922c
9839629 99641 0 None 1 2 Human 11.0 pKi = 11 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 309 5 1 3 3.8 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL287560 99641 0 None 1 2 Human 11.0 pKi = 11 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 309 5 1 3 3.8 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
10925712 112075 0 None 1 2 Human 11.0 pKi = 11 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 335 7 1 3 4.3 C=CCC(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL330137 112075 0 None 1 2 Human 11.0 pKi = 11 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 335 7 1 3 4.3 C=CCC(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
9839629 99641 0 None 1 2 Human 11.0 pKi = 11 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 mins
ChEMBL 309 5 1 3 3.8 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.5b00982
CHEMBL287560 99641 0 None 1 2 Human 11.0 pKi = 11 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 mins
ChEMBL 309 5 1 3 3.8 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.5b00982
9796846 115923 0 None 12 2 Human 10.9 pKi = 10.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 313 5 1 3 3.4 CCC(=O)NCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL336054 115923 0 None 12 2 Human 10.9 pKi = 10.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 313 5 1 3 3.4 CCC(=O)NCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
53237947 61671 0 None -1 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 299 5 1 2 3.5 CCC(=O)NCCC1=C(C(C)C)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774514 61671 0 None -1 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 299 5 1 2 3.5 CCC(=O)NCCC1=C(C(C)C)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
115348 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
1343 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
CHEMBL289233 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
DB08190 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
1356 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
208902 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
2355 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
CHEMBL1218 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
DB00980 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
1356 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
208902 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
2355 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
CHEMBL1218 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
DB00980 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
9926304 116062 0 None 9 2 Human 10.8 pKi = 10.8 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 299 4 1 3 3.0 COc1ccc2ccc(OC)c3c2c1CCC3CNC(C)=O 10.1021/jm000922c
CHEMBL336509 116062 0 None 9 2 Human 10.8 pKi = 10.8 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 299 4 1 3 3.0 COc1ccc2ccc(OC)c3c2c1CCC3CNC(C)=O 10.1021/jm000922c
9797460 117637 0 None 6 2 Human 10.8 pKi = 10.8 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 327 6 1 3 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL340832 117637 0 None 6 2 Human 10.8 pKi = 10.8 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 327 6 1 3 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
11723593 106382 0 None -1 2 Human 10.7 pKi = 10.7 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 321 6 1 3 4.0 C=CC(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL314512 106382 0 None -1 2 Human 10.7 pKi = 10.7 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 321 6 1 3 4.0 C=CC(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
53237946 61670 0 None -1 2 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 285 4 1 2 3.1 CC(=O)NCCC1=C(C(C)C)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774513 61670 0 None -1 2 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 285 4 1 2 3.1 CC(=O)NCCC1=C(C(C)C)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
9840277 23345 0 None 10 2 Human 10.6 pKi = 10.6 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 325 5 1 3 3.4 COc1ccc2ccc(OC)c3c2c1CCC3CNC(=O)C1CC1 10.1021/jm000922c
CHEMBL133416 23345 0 None 10 2 Human 10.6 pKi = 10.6 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 325 5 1 3 3.4 COc1ccc2ccc(OC)c3c2c1CCC3CNC(=O)C1CC1 10.1021/jm000922c
53310841 63451 0 None 5 2 Human 10.6 pKi = 10.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 299 5 1 4 2.2 CCC(=O)NCCc1c(C2CC2)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802028 63451 0 None 5 2 Human 10.6 pKi = 10.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 299 5 1 4 2.2 CCC(=O)NCCc1c(C2CC2)nn2ccc3c(c12)CCO3 10.1021/jm200385u
164621472 185303 0 None 2 2 Human 10.6 pKi = 10.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 288 4 1 3 3.6 CCC(=O)NCCC1CCc2ccc3nc(C)sc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4868554 185303 0 None 2 2 Human 10.6 pKi = 10.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 288 4 1 3 3.6 CCC(=O)NCCC1CCc2ccc3nc(C)sc3c21 10.1021/acs.jmedchem.0c01836
9873402 35596 0 None 1 2 Human 10.5 pKi = 10.5 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 596 19 2 4 7.9 CC(=O)NCCc1cccc2ccc(OCCCCCCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
CHEMBL14417 35596 0 None 1 2 Human 10.5 pKi = 10.5 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 596 19 2 4 7.9 CC(=O)NCCc1cccc2ccc(OCCCCCCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
18466111 19630 0 None 1 2 Human 10.5 pKi = 10.5 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL130214 19630 0 None 1 2 Human 10.5 pKi = 10.5 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
122188346 122633 0 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 262 4 1 3 2.0 CCC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612603 122633 0 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 262 4 1 3 2.0 CCC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
71533431 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 10.1016/j.bmcl.2012.11.069
7775 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 10.1016/j.bmcl.2012.11.069
CHEMBL2314259 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 10.1016/j.bmcl.2012.11.069
57781216 125313 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648356 125313 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
53237949 61673 0 None -3 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 339 4 1 2 3.7 CC(C)C1=C(CCNC(=O)C(F)(F)F)c2c(ccc3c2CCO3)C1 10.1021/jm200221q
CHEMBL1774516 61673 0 None -3 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 339 4 1 2 3.7 CC(C)C1=C(CCNC(=O)C(F)(F)F)c2c(ccc3c2CCO3)C1 10.1021/jm200221q
23725567 125319 0 None 2 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 274 3 1 3 3.2 CC(=O)NCCC1CCc2ccc3nc(C)sc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648362 125319 0 None 2 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 274 3 1 3 3.2 CC(=O)NCCC1CCc2ccc3nc(C)sc3c21 10.1021/acs.jmedchem.0c01836
24954990 63449 0 None 5 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 287 5 1 4 1.9 CCC(=O)NCCc1c(CC)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802026 63449 0 None 5 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 287 5 1 4 1.9 CCC(=O)NCCc1c(CC)nn2ccc3c(c12)CCO3 10.1021/jm200385u
10925379 205821 0 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 324 5 2 3 3.6 CNC(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL94838 205821 0 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 324 5 2 3 3.6 CNC(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
56659223 64643 0 None 5 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 2 3 2.9 COc1ccc2[nH]c(-c3ccccc3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2011.06.030
CHEMBL1823015 64643 0 None 5 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 2 3 2.9 COc1ccc2[nH]c(-c3ccccc3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2011.06.030
127042142 137534 0 None 3 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 310 5 1 4 3.2 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3765540 137534 0 None 3 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 310 5 1 4 3.2 COc1ccc2oc(-c3ccccc3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
71533430 85973 0 None -1 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 241 3 1 2 3.0 COc1ccc2cccc(/C=C/NC(C)=O)c2c1 10.1016/j.bmcl.2012.11.069
CHEMBL2314255 85973 0 None -1 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 241 3 1 2 3.0 COc1ccc2cccc(/C=C/NC(C)=O)c2c1 10.1016/j.bmcl.2012.11.069
53310840 63450 0 None 6 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 285 4 1 4 1.8 CC(=O)NCCc1c(C2CC2)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802027 63450 0 None 6 2 Human 10.4 pKi = 10.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 285 4 1 4 1.8 CC(=O)NCCc1c(C2CC2)nn2ccc3c(c12)CCO3 10.1021/jm200385u
22004791 61669 0 None -2 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 243 3 1 2 2.1 CC(=O)NCCC1=CCc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774512 61669 0 None -2 2 Human 10.4 pKi = 10.4 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 243 3 1 2 2.1 CC(=O)NCCC1=CCc2ccc3c(c21)CCO3 10.1021/jm200221q
9916005 32478 0 None 3 2 Human 10.3 pKi = 10.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 568 17 2 4 7.1 CC(=O)NCCc1cccc2ccc(OCCCCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
CHEMBL14136 32478 0 None 3 2 Human 10.3 pKi = 10.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 568 17 2 4 7.1 CC(=O)NCCc1cccc2ccc(OCCCCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
9914839 97691 0 None 34 2 Human 10.3 pKi = 10.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 526 14 2 4 6.0 CC(=O)NCCc1cccc2ccc(OCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
CHEMBL273787 97691 0 None 34 2 Human 10.3 pKi = 10.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 526 14 2 4 6.0 CC(=O)NCCc1cccc2ccc(OCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
44264903 203896 0 None 4 2 Human 10.3 pKi = 10.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 270 4 1 3 3.4 COc1cccc(N(C)c2ccc(NC(C)=O)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL8168 203896 0 None 4 2 Human 10.3 pKi = 10.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 270 4 1 3 3.4 COc1cccc(N(C)c2ccc(NC(C)=O)cc2)c1 10.1016/j.bmcl.2003.11.030
44272316 67243 0 None 4 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 392 10 2 3 5.3 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CCCCc1ccccc1)N2 10.1016/j.bmcl.2003.12.052
CHEMBL19026 67243 0 None 4 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 392 10 2 3 5.3 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CCCCc1ccccc1)N2 10.1016/j.bmcl.2003.12.052
10452167 78364 0 None 1 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 376 9 1 3 5.0 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2003.12.052
CHEMBL2112690 78364 0 None 1 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 376 9 1 3 5.0 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2003.12.052
9998754 78369 0 None 7 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 362 8 1 3 4.6 CC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2003.12.052
CHEMBL2112700 78369 0 None 7 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 362 8 1 3 4.6 CC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2003.12.052
10446712 78373 0 None 6 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 286 6 1 3 3.4 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CC)oc12 10.1016/j.bmcl.2003.12.052
CHEMBL2112722 78373 0 None 6 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 286 6 1 3 3.4 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CC)oc12 10.1016/j.bmcl.2003.12.052
10016733 78374 0 None 3 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 284 5 1 3 3.0 CCc1nc2cccc([C@@H]3C[C@H]3CNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2003.12.052
CHEMBL2112724 78374 0 None 3 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 284 5 1 3 3.0 CCc1nc2cccc([C@@H]3C[C@H]3CNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2003.12.052
10423378 78375 0 None 8 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 272 5 1 3 3.0 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CC)oc12 10.1016/j.bmcl.2003.12.052
CHEMBL2112727 78375 0 None 8 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 272 5 1 3 3.0 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2nc(CC)oc12 10.1016/j.bmcl.2003.12.052
11741001 78379 0 None 9 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 388 9 1 3 5.0 O=C(NC[C@@H]1C[C@H]1c1cccc2nc(CCCCc3ccccc3)oc12)C1CC1 10.1016/j.bmcl.2003.12.052
CHEMBL2112734 78379 0 None 9 2 Human 10.3 pKi = 10.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 388 9 1 3 5.0 O=C(NC[C@@H]1C[C@H]1c1cccc2nc(CCCCc3ccccc3)oc12)C1CC1 10.1016/j.bmcl.2003.12.052
57381112 1383 0 None 20 2 Human 10.3 pKi = 10.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 10.1039/C5MD00190K
7776 1383 0 None 20 2 Human 10.3 pKi = 10.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 10.1039/C5MD00190K
CHEMBL1946221 1383 0 None 20 2 Human 10.3 pKi = 10.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 10.1039/C5MD00190K
57381112 1383 0 None 20 2 Human 10.3 pKi = 10.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 10.1039/C5MD00190K
7776 1383 0 None 20 2 Human 10.3 pKi = 10.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 10.1039/C5MD00190K
CHEMBL1946221 1383 0 None 20 2 Human 10.3 pKi = 10.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 10.1039/C5MD00190K
9798080 19270 0 None 3 2 Human 10.2 pKi = 10.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 341 7 1 3 4.2 CCCC(=O)NCCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL129890 19270 0 None 3 2 Human 10.2 pKi = 10.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 341 7 1 3 4.2 CCCC(=O)NCCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
53238407 61681 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 349 5 1 3 3.6 COc1cccc(C2=C(CCNC(C)=O)c3c(ccc4c3CCO4)C2)c1 10.1021/jm200221q
CHEMBL1774526 61681 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 349 5 1 3 3.6 COc1cccc(C2=C(CCNC(C)=O)c3c(ccc4c3CCO4)C2)c1 10.1021/jm200221q
198 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
82148 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
99 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
CHEMBL10878 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
DB06594 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
198 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
82148 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
99 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
CHEMBL10878 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
DB06594 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
15453090 85971 0 None 3 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 285 4 1 3 2.8 COc1ccc2ccc(OC)c([C@@H]3C[C@H]3NC(C)=O)c2c1 10.1016/j.bmcl.2012.11.069
CHEMBL2314253 85971 0 None 3 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 285 4 1 3 2.8 COc1ccc2ccc(OC)c([C@@H]3C[C@H]3NC(C)=O)c2c1 10.1016/j.bmcl.2012.11.069
24954989 1497 1 None 6 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 10.1021/jm200385u
7774 1497 1 None 6 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 10.1021/jm200385u
CHEMBL1802025 1497 1 None 6 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 10.1021/jm200385u
23725565 125312 0 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCCC1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648355 125312 0 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCCC1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
23725514 125315 0 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 272 4 1 3 3.1 CCC(=O)NCCC1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648358 125315 0 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 272 4 1 3 3.1 CCC(=O)NCCC1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
115348 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
1343 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
CHEMBL289233 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
DB08190 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
53238185 61679 0 None -2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 320 4 1 3 3.0 CC(=O)NCCC1=C(c2cccnc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774524 61679 0 None -2 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 320 4 1 3 3.0 CC(=O)NCCC1=C(c2cccnc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
9883864 116141 0 None 7 2 Human 10.2 pKi = 10.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 327 6 1 3 3.8 CCC(=O)NCCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL337024 116141 0 None 7 2 Human 10.2 pKi = 10.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 327 6 1 3 3.8 CCC(=O)NCCC1CCc2c(OC)ccc3ccc(OC)c1c23 10.1021/jm000922c
46888521 8542 0 None 26 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 499 12 1 5 5.6 COC(=O)Cc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095196 8542 0 None 26 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 499 12 1 5 5.6 COC(=O)Cc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
1351 2353 15 None -1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 10.1039/C4MD00149D
219018 2353 15 None -1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 10.1039/C4MD00149D
CHEMBL4079759 2353 15 None -1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 10.1039/C4MD00149D
9893513 30730 0 None 29 2 Human 10.1 pKi = 10.1 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 540 15 2 4 6.4 CC(=O)NCCc1cccc2ccc(OCCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
CHEMBL13985 30730 0 None 29 2 Human 10.1 pKi = 10.1 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 540 15 2 4 6.4 CC(=O)NCCc1cccc2ccc(OCCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
115348 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
1343 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
CHEMBL289233 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
DB08190 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
11100761 101308 4 None -1 2 Human 10.1 pKi = 10.1 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 372 4 1 3 2.5 COc1ccc2c(c1)c(CCNC(C)=O)c(I)n2C 10.1021/jm011053+
CHEMBL300056 101308 4 None -1 2 Human 10.1 pKi = 10.1 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 372 4 1 3 2.5 COc1ccc2c(c1)c(CCNC(C)=O)c(I)n2C 10.1021/jm011053+
1357 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970437q
1672 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970437q
224 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970437q
896 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970437q
CHEMBL45 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970437q
DB01065 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970437q
24955343 63446 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 321 4 1 4 2.6 CC(=O)NCCc1c(-c2ccccc2)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802022 63446 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 321 4 1 4 2.6 CC(=O)NCCc1c(-c2ccccc2)nn2ccc3c(c12)CCO3 10.1021/jm200385u
1357 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0201159
1672 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0201159
224 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0201159
896 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0201159
CHEMBL45 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0201159
DB01065 2440 133 None -1 9 Human 10.1 pKi = 10.1 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0201159
53310839 63448 0 None 2 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.6 CCC(=O)NCCc1c(C)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802024 63448 0 None 2 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 273 4 1 4 1.6 CCC(=O)NCCc1c(C)nn2ccc3c(c12)CCO3 10.1021/jm200385u
10163052 8421 0 None 72 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 483 12 2 4 5.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc(-c4ccc(CO)cc4)cc3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1094212 8421 0 None 72 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 483 12 2 4 5.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc(-c4ccc(CO)cc4)cc3)cc12 10.1016/j.bmc.2010.04.008
1357 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1672 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
224 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
896 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
CHEMBL45 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
DB01065 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1357 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.09.003
1672 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.09.003
224 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.09.003
896 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.09.003
CHEMBL45 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.09.003
DB01065 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.09.003
10016919 100131 1 None 3 2 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 287 6 1 3 2.9 CCC(=O)NCCc1c(OC)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
CHEMBL291857 100131 1 None 3 2 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 287 6 1 3 2.9 CCC(=O)NCCc1c(OC)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
10016919 100131 1 None 3 2 Human 10.0 pKi = 10 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 287 6 1 3 2.9 CCC(=O)NCCc1c(OC)ccc2ccc(OC)cc12 10.1021/jm970437q
CHEMBL291857 100131 1 None 3 2 Human 10.0 pKi = 10 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 287 6 1 3 2.9 CCC(=O)NCCc1c(OC)ccc2ccc(OC)cc12 10.1021/jm970437q
10659603 20041 0 None -1 2 Human 10.0 pKi = 10 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 4 1 2 3.0 CCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL130542 20041 0 None -1 2 Human 10.0 pKi = 10 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 4 1 2 3.0 CCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
9925797 22037 0 None 3 2 Human 10.0 pKi = 10 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 4 1 2 3.4 COc1ccc2cccc3c2c1C(CCNC(C)=O)CC3 10.1021/jm000922c
CHEMBL132340 22037 0 None 3 2 Human 10.0 pKi = 10 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 4 1 2 3.4 COc1ccc2cccc3c2c1C(CCNC(C)=O)CC3 10.1021/jm000922c
198 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
82148 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
99 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
CHEMBL10878 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
DB06594 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
145982070 165911 0 None 1 2 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 283 3 1 2 3.2 COc1ccc2ccc3c(c2c1)C(C)(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4278248 165911 0 None 1 2 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 283 3 1 2 3.2 COc1ccc2ccc3c(c2c1)C(C)(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
198 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
82148 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
99 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
CHEMBL10878 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
DB06594 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
198 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
82148 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
99 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
CHEMBL10878 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
DB06594 310 120 None -1 6 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
71540389 85974 0 None -1 2 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 241 3 1 2 3.0 COc1ccc2ccccc2c1/C=C/NC(C)=O 10.1016/j.bmcl.2012.11.069
CHEMBL2314257 85974 0 None -1 2 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 241 3 1 2 3.0 COc1ccc2ccccc2c1/C=C/NC(C)=O 10.1016/j.bmcl.2012.11.069
9839199 21148 0 None -1 2 Human 10.0 pKi = 10.0 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
CHEMBL131424 21148 0 None -1 2 Human 10.0 pKi = 10.0 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
53237948 61672 0 None -3 2 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 311 5 1 2 3.5 CC(C)C1=C(CCNC(=O)C2CC2)c2c(ccc3c2CCO3)C1 10.1021/jm200221q
CHEMBL1774515 61672 0 None -3 2 Human 10.0 pKi = 10.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 311 5 1 2 3.5 CC(C)C1=C(CCNC(=O)C2CC2)c2c(ccc3c2CCO3)C1 10.1021/jm200221q
1357 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
1672 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
224 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
896 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
CHEMBL45 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
DB01065 2440 133 None -1 9 Human 10.0 pKi = 10.0 Binding
Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm8007618
10562968 19980 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 255 3 1 2 2.6 COc1ccc2cccc3c2c1C(CNC(C)=O)C3 10.1021/jm000922c
CHEMBL130490 19980 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 255 3 1 2 2.6 COc1ccc2cccc3c2c1C(CNC(C)=O)C3 10.1021/jm000922c
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
198 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
82148 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
99 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
CHEMBL10878 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
DB06594 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.12.013
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.12.013
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.12.013
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.12.013
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.12.013
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.12.013
198 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
82148 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
99 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
CHEMBL10878 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
DB06594 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm011053+
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm011053+
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm011053+
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm011053+
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm011053+
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm011053+
198 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
82148 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
99 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
CHEMBL10878 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
DB06594 310 120 None -1 6 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00392-2
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00392-2
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00392-2
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00392-2
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00392-2
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00392-2
44272305 66971 0 None 14 2 Human 9.9 pKi = 9.9 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 392 9 2 3 5.1 CC(C)C(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CCCCc1ccccc1)N2 10.1016/j.bmcl.2003.12.052
CHEMBL18845 66971 0 None 14 2 Human 9.9 pKi = 9.9 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 392 9 2 3 5.1 CC(C)C(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CCCCc1ccccc1)N2 10.1016/j.bmcl.2003.12.052
44358146 26855 0 None 2 2 Human 9.9 pKi = 9.9 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 4 1 3 2.1 CCCC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL136531 26855 0 None 2 2 Human 9.9 pKi = 9.9 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 4 1 3 2.1 CCCC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.08.052
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.08.052
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.08.052
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.08.052
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.08.052
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.08.052
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2014.09.038
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2014.09.038
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2014.09.038
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2014.09.038
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2014.09.038
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2014.09.038
1357 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm700957j
1672 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm700957j
224 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm700957j
896 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm700957j
CHEMBL45 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm700957j
DB01065 2440 133 None -1 9 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm700957j
10059864 109322 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL323332 109322 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm0005252
56653119 171216 0 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 322 7 2 2 3.5 CC(=O)NCCc1c[nH]c2ccc(OCCc3ccccc3)cc12 10.1016/j.ejmech.2019.111847
CHEMBL4467954 171216 0 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 322 7 2 2 3.5 CC(=O)NCCc1c[nH]c2ccc(OCCc3ccccc3)cc12 10.1016/j.ejmech.2019.111847
10059864 109322 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL323332 109322 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2015.12.047
10059864 109322 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2016.01.008
CHEMBL323332 109322 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2016.01.008
24954991 63447 0 None 3 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 259 3 1 4 1.3 CC(=O)NCCc1c(C)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802023 63447 0 None 3 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 259 3 1 4 1.3 CC(=O)NCCc1c(C)nn2ccc3c(c12)CCO3 10.1021/jm200385u
1357 2440 133 None -1 9 Human 9.8 pKi = 9.8 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm020982d
1672 2440 133 None -1 9 Human 9.8 pKi = 9.8 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm020982d
224 2440 133 None -1 9 Human 9.8 pKi = 9.8 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm020982d
896 2440 133 None -1 9 Human 9.8 pKi = 9.8 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm020982d
CHEMBL45 2440 133 None -1 9 Human 9.8 pKi = 9.8 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm020982d
DB01065 2440 133 None -1 9 Human 9.8 pKi = 9.8 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm020982d
25025104 185723 0 None 5 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 271 4 1 3 2.6 CCC(=O)NCCC1CCc2ccn3nc(C)cc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4874630 185723 0 None 5 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 271 4 1 3 2.6 CCC(=O)NCCC1CCc2ccn3nc(C)cc3c21 10.1021/acs.jmedchem.0c01836
44358196 118768 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 260 3 1 3 1.7 CCC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL343825 118768 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 260 3 1 3 1.7 CCC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
198 310 120 None -1 6 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
82148 310 120 None -1 6 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
99 310 120 None -1 6 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
CHEMBL10878 310 120 None -1 6 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
DB06594 310 120 None -1 6 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
44272317 98443 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 300 6 2 3 3.2 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C3CC3)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL279343 98443 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 300 6 2 3 3.2 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C3CC3)c2O1 10.1016/j.bmcl.2003.12.052
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
9817262 19269 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 4 1 2 3.4 CCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
CHEMBL129889 19269 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 4 1 2 3.4 CCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm000922c
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm000922c
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm000922c
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm000922c
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm000922c
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm000922c
9948714 20489 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 313 5 1 3 3.4 COc1ccc2ccc(OC)c3c2c1CCC3CCNC(C)=O 10.1021/jm000922c
CHEMBL130898 20489 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 313 5 1 3 3.4 COc1ccc2ccc(OC)c3c2c1CCC3CCNC(C)=O 10.1021/jm000922c
44272422 167305 0 None 3 2 Human 9.7 pKi = 9.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 288 5 2 3 3.1 CCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C(C)C)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL431103 167305 0 None 3 2 Human 9.7 pKi = 9.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 288 5 2 3 3.1 CCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C(C)C)c2O1 10.1016/j.bmcl.2003.12.052
21581654 60413 1 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760944 60413 1 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00444-7
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00444-7
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00444-7
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00444-7
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00444-7
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/S0960-894X(97)00444-7
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.03.080
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.03.080
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.03.080
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.03.080
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.03.080
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.03.080
59145922 185680 0 None 7 2 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 257 3 1 3 2.2 CC(=O)NCCC1CCc2ccn3nc(C)cc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4874010 185680 0 None 7 2 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 257 3 1 3 2.2 CC(=O)NCCC1CCc2ccn3nc(C)cc3c21 10.1021/acs.jmedchem.0c01836
127042442 137372 0 None -6 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 328 5 1 4 3.3 COc1ccc2oc(-c3ccc(F)cc3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3763503 137372 0 None -6 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 328 5 1 4 3.3 COc1ccc2oc(-c3ccc(F)cc3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
127042791 137519 0 None -2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 360 4 1 4 2.1 COc1ccc2oc(I)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3765401 137519 0 None -2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 360 4 1 4 2.1 COc1ccc2oc(I)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2012.11.069
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2012.11.069
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2012.11.069
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2012.11.069
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2012.11.069
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2012.11.069
71540396 85976 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 286 4 2 3 2.8 CNC(=O)N/C=C/c1c(OC)ccc2ccc(OC)cc12 10.1016/j.bmcl.2012.11.069
CHEMBL2314260 85976 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 286 4 2 3 2.8 CNC(=O)N/C=C/c1c(OC)ccc2ccc(OC)cc12 10.1016/j.bmcl.2012.11.069
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.8b00893
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.8b00893
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.8b00893
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.8b00893
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.8b00893
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.8b00893
10540964 116115 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCC(=O)NCCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL336858 116115 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCC(=O)NCCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
44272320 98137 0 None -2 2 Human 9.7 pKi = 9.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 288 6 2 3 3.2 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)CC)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL276921 98137 0 None -2 2 Human 9.7 pKi = 9.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 288 6 2 3 3.2 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)CC)c2O1 10.1016/j.bmcl.2003.12.052
1357 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.044
1672 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.044
224 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.044
896 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.044
CHEMBL45 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.044
DB01065 2440 133 None -1 9 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.02.044
23725515 125322 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 272 4 1 3 2.9 CCc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 10.1021/acs.jmedchem.0c01836
CHEMBL3648365 125322 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 272 4 1 3 2.9 CCc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 10.1021/acs.jmedchem.0c01836
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.12.047
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.12.047
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.12.047
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.12.047
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.12.047
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2015.12.047
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
21581654 60413 1 None 1 2 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2011.06.030
CHEMBL1760944 60413 1 None 1 2 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2011.06.030
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
21581654 60413 1 None 1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL1760944 60413 1 None 1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 2 3 1.3 COc1ccc2[nH]cc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.06.030
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.06.030
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.06.030
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.06.030
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.06.030
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2011.06.030
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.01.008
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.01.008
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.01.008
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.01.008
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.01.008
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.01.008
18360631 8612 0 None 26 2 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 516 13 2 4 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4c(c3)C(CCNC(C)=O)CCC4)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095831 8612 0 None 26 2 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 516 13 2 4 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4c(c3)C(CCNC(C)=O)CCC4)cc12 10.1016/j.bmc.2010.04.008
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2011.06.063
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2011.06.063
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2011.06.063
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2011.06.063
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2011.06.063
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2011.06.063
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.04.013
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.04.013
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.04.013
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.04.013
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.04.013
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2007.04.013
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2020.112090
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2020.112090
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2020.112090
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2020.112090
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2020.112090
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2020.112090
1357 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
1672 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
224 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
896 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
CHEMBL45 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
DB01065 2440 133 None -1 9 Human 9.6 pKi = 9.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm040768k
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm040768k
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm040768k
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm040768k
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm040768k
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm040768k
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm001125h
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm001125h
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm001125h
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm001125h
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm001125h
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm001125h
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm048956y
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm048956y
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm048956y
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm048956y
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm048956y
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm048956y
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970721h
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970721h
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970721h
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970721h
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970721h
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm970721h
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2012.10.060
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2012.10.060
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2012.10.060
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2012.10.060
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2012.10.060
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2012.10.060
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2010.02.084
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2010.02.084
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2010.02.084
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2010.02.084
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2010.02.084
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2010.02.084
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2005.01.015
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2005.01.015
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2005.01.015
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2005.01.015
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2005.01.015
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2005.01.015
145981162 165933 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 270 3 2 2 2.5 COc1ccc2ccc3c(c2c1)C(CNC(N)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4278575 165933 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 270 3 2 2 2.5 COc1ccc2ccc3c(c2c1)C(CNC(N)=O)CC3 10.1016/j.ejmech.2017.10.025
145986532 166717 0 None -1 3 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 269 3 1 2 3.0 COc1ccc2ccc3c(c2c1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4293386 166717 0 None -1 3 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 269 3 1 2 3.0 COc1ccc2ccc3c(c2c1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
137660333 158961 0 None -1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 COc1ccc2cccc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4102177 158961 0 None -1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 COc1ccc2cccc(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.12.013
25024912 185327 0 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 271 4 1 3 2.5 CCC(=O)NCCC1CCc2ccc3nn(C)cc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4869029 185327 0 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 271 4 1 3 2.5 CCC(=O)NCCC1CCc2ccc3nn(C)cc3c21 10.1021/acs.jmedchem.0c01836
15453084 85969 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 255 3 1 2 2.8 COc1ccc2cccc([C@@H]3C[C@H]3NC(C)=O)c2c1 10.1016/j.bmcl.2012.11.069
CHEMBL2314251 85969 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 255 3 1 2 2.8 COc1ccc2cccc([C@@H]3C[C@H]3NC(C)=O)c2c1 10.1016/j.bmcl.2012.11.069
11079938 192890 4 None -1 2 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 403 5 2 4 2.4 COc1cc2c(CCNC(C)=O)c(I)[nH]c2cc1[N+](=O)[O-] 10.1021/jm011053+
CHEMBL52755 192890 4 None -1 2 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 403 5 2 4 2.4 COc1cc2c(CCNC(C)=O)c(I)[nH]c2cc1[N+](=O)[O-] 10.1021/jm011053+
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.07.055
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.07.055
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.07.055
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.07.055
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.07.055
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.07.055
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jnatprod.7b00853
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jnatprod.7b00853
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jnatprod.7b00853
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jnatprod.7b00853
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jnatprod.7b00853
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jnatprod.7b00853
53310987 63453 0 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 327 4 1 4 2.4 CCC(=O)NCCc1c(C(F)(F)F)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802030 63453 0 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 327 4 1 4 2.4 CCC(=O)NCCc1c(C(F)(F)F)nn2ccc3c(c12)CCO3 10.1021/jm200385u
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm060850a
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm060850a
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm060850a
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm060850a
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm060850a
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm060850a
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.06.100
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.06.100
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.06.100
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.06.100
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.06.100
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.06.100
139451781 184265 0 None -1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 289 5 1 5 1.5 CCOc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
CHEMBL4852440 184265 0 None -1 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 289 5 1 5 1.5 CCOc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
1357 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
1672 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
224 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
896 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
CHEMBL45 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
DB01065 2440 133 None -1 9 Human 9.5 pKi = 9.5 Binding
Binding affinity to human MT1A receptor by radioligand displacement assayBinding affinity to human MT1A receptor by radioligand displacement assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2013.01.044
44272440 67171 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 260 4 2 3 2.5 CCC1Nc2cccc([C@@H]3C[C@H]3CNC(C)=O)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL18960 67171 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 260 4 2 3 2.5 CCC1Nc2cccc([C@@H]3C[C@H]3CNC(C)=O)c2O1 10.1016/j.bmcl.2003.12.052
59145872 185584 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 257 3 1 3 2.1 CC(=O)NCCC1CCc2ccc3nn(C)cc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4872592 185584 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 257 3 1 3 2.1 CC(=O)NCCC1CCc2ccc3nn(C)cc3c21 10.1021/acs.jmedchem.0c01836
18466111 19630 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL130214 19630 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
10661735 167750 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 6 1 2 3.8 CCCC(=O)NCCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL434226 167750 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 6 1 2 3.8 CCCC(=O)NCCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
46888522 8543 0 None 11 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 513 12 1 5 6.2 COC(=O)C(C)c1ccc2cc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)ccc2c1 10.1016/j.bmc.2010.04.008
CHEMBL1095197 8543 0 None 11 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 513 12 1 5 6.2 COC(=O)C(C)c1ccc2cc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)ccc2c1 10.1016/j.bmc.2010.04.008
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptorDisplacement of [125I]2-iodomelatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm2006782
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptorDisplacement of [125I]2-iodomelatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm2006782
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptorDisplacement of [125I]2-iodomelatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm2006782
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptorDisplacement of [125I]2-iodomelatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm2006782
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptorDisplacement of [125I]2-iodomelatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm2006782
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptorDisplacement of [125I]2-iodomelatonin from human MT1 receptor
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm2006782
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2007.01.005
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2007.01.005
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2007.01.005
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2007.01.005
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2007.01.005
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2007.01.005
139451763 185741 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 305 8 1 5 2.4 CCCC(=O)NCCn1c(OCC)nc2ccc(OC)cc21 10.1021/acs.jmedchem.0c00627
CHEMBL4874954 185741 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 305 8 1 5 2.4 CCCC(=O)NCCn1c(OCC)nc2ccc(OC)cc21 10.1021/acs.jmedchem.0c00627
44317845 203785 0 None 3 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 301 7 1 3 3.3 CCOc1ccc2ccc(OC)cc2c1CCNC(=O)CC 10.1016/S0960-894X(97)00444-7
CHEMBL80736 203785 0 None 3 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 301 7 1 3 3.3 CCOc1ccc2ccc(OC)cc2c1CCNC(=O)CC 10.1016/S0960-894X(97)00444-7
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0512544
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0512544
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0512544
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0512544
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0512544
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0512544
57781246 125323 0 None -2 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 284 4 1 3 3.3 CC(=O)NCCC1CCc2ccc3nc(C4CC4)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648366 125323 0 None -2 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 284 4 1 3 3.3 CC(=O)NCCC1CCc2ccc3nc(C4CC4)oc3c21 10.1021/acs.jmedchem.0c01836
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.09.030
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.09.030
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.09.030
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.09.030
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.09.030
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.09.030
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.04.082
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.04.082
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.04.082
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.04.082
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.04.082
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2004.04.082
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.12.052
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.12.052
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.12.052
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.12.052
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.12.052
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.12.052
145982333 165993 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4279639 165993 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145981769 166103 0 None -1 3 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 270 3 1 3 2.4 COc1ccc2ccc3c(c2n1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4281712 166103 0 None -1 3 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 270 3 1 3 2.4 COc1ccc2ccc3c(c2n1)C(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
10778397 19620 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 4 1 2 3.0 COc1ccc2cccc3c2c1C(CCNC(C)=O)C3 10.1021/jm000922c
CHEMBL130203 19620 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 4 1 2 3.0 COc1ccc2cccc3c2c1C(CCNC(C)=O)C3 10.1021/jm000922c
139451795 184737 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 277 6 1 5 1.6 CCOc1nc2ccc(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859677 184737 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 277 6 1 5 1.6 CCOc1nc2ccc(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
9839199 21148 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
CHEMBL131424 21148 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
57781227 125311 0 None -6 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 244 3 1 3 2.4 CC(=O)NCCC1CCc2ccc3ncoc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648354 125311 0 None -6 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 244 3 1 3 2.4 CC(=O)NCCC1CCc2ccc3ncoc3c21 10.1021/acs.jmedchem.0c01836
23725612 125324 0 None -2 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 274 4 1 4 2.4 COc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 10.1021/acs.jmedchem.0c01836
CHEMBL3648367 125324 0 None -2 2 Human 9.4 pKi = 9.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 274 4 1 4 2.4 COc1nc2ccc3c(c2o1)C(CCNC(C)=O)CC3 10.1021/acs.jmedchem.0c01836
1357 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C1MD00149C
1672 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C1MD00149C
224 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C1MD00149C
896 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C1MD00149C
CHEMBL45 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C1MD00149C
DB01065 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C1MD00149C
1357 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
1672 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
224 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
896 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
CHEMBL45 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
DB01065 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1039/C5MD00190K
1357 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm800974d
1672 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm800974d
224 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm800974d
896 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm800974d
CHEMBL45 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm800974d
DB01065 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm800974d
1357 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2009.04.068
1672 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2009.04.068
224 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2009.04.068
896 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2009.04.068
CHEMBL45 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2009.04.068
DB01065 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2009.04.068
1357 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1672 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
224 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
896 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
CHEMBL45 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
DB01065 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
24954992 63452 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 313 3 1 4 2.0 CC(=O)NCCc1c(C(F)(F)F)nn2ccc3c(c12)CCO3 10.1021/jm200385u
CHEMBL1802029 63452 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 313 3 1 4 2.0 CC(=O)NCCc1c(C(F)(F)F)nn2ccc3c(c12)CCO3 10.1021/jm200385u
1362 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
9870523 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
CHEMBL429392 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
1362 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9870523 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL429392 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
1362 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9870523 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL429392 3370 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
1357 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.07.012
1672 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.07.012
224 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.07.012
896 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.07.012
CHEMBL45 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.07.012
DB01065 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2008.07.012
1357 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.11.030
1672 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.11.030
224 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.11.030
896 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.11.030
CHEMBL45 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.11.030
DB01065 2440 133 None -1 9 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2003.11.030
7778 799 0 None 97 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 10.1016/j.bmc.2010.04.008
9957516 799 0 None 97 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 10.1016/j.bmc.2010.04.008
CHEMBL1094546 799 0 None 97 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 10.1016/j.bmc.2010.04.008
1355 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
9806449 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
CHEMBL14453 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
1355 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9806449 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL14453 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
44272425 66975 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 300 5 2 3 3.1 CC(C)C1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C3CC3)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL18846 66975 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 300 5 2 3 3.1 CC(C)C1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C3CC3)c2O1 10.1016/j.bmcl.2003.12.052
1355 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9806449 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL14453 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
145982333 165993 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4279639 165993 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145993188 166458 0 None -3 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 319 4 1 3 2.6 COc1ccc2ccc3c(c2c1)C(C)(CNS(C)(=O)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4288497 166458 0 None -3 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 319 4 1 3 2.6 COc1ccc2ccc3c(c2c1)C(C)(CNS(C)(=O)=O)CC3 10.1016/j.ejmech.2017.10.025
145988741 166672 0 None -6 3 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 299 5 1 3 2.6 COCC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4292336 166672 0 None -6 3 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 299 5 1 3 2.6 COCC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
1355 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
9806449 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
CHEMBL14453 3371 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
137647756 157389 0 None -6 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 259 4 2 3 1.7 CNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4084612 157389 0 None -6 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 259 4 2 3 1.7 CNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
139451764 185675 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 275 4 1 5 1.1 COc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
CHEMBL4873903 185675 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 275 4 1 5 1.1 COc1nc2ccc3c(c2n1CCNC(C)=O)CCO3 10.1021/acs.jmedchem.0c00627
44349100 114300 0 None 34 2 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 376 10 1 3 4.9 O=C(NCCCc1cccc2nc(CCCCc3ccccc3)oc12)C1CC1 10.1016/j.bmcl.2004.04.082
CHEMBL334079 114300 0 None 34 2 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 376 10 1 3 4.9 O=C(NCCCc1cccc2nc(CCCCc3ccccc3)oc12)C1CC1 10.1016/j.bmcl.2004.04.082
44349100 114300 0 None 34 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 10 1 3 4.9 O=C(NCCCc1cccc2nc(CCCCc3ccccc3)oc12)C1CC1 10.1021/jm401343c
CHEMBL334079 114300 0 None 34 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 10 1 3 4.9 O=C(NCCCc1cccc2nc(CCCCc3ccccc3)oc12)C1CC1 10.1021/jm401343c
46888492 8740 0 None 18 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 564 14 2 5 6.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)c5ccco5)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1096991 8740 0 None 18 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 564 14 2 5 6.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)c5ccco5)c4c3)cc12 10.1016/j.bmc.2010.04.008
10468642 26896 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 275 3 2 3 1.5 CCNC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL136564 26896 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 275 3 2 3 1.5 CCNC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
10640828 21267 0 None 2 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 339 6 1 3 3.8 COc1ccc2ccc(OC)c3c2c1CCC3CCNC(=O)C1CC1 10.1021/jm000922c
CHEMBL131575 21267 0 None 2 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 339 6 1 3 3.8 COc1ccc2ccc(OC)c3c2c1CCC3CCNC(=O)C1CC1 10.1021/jm000922c
1357 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980684+
1672 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980684+
224 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980684+
896 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980684+
CHEMBL45 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980684+
DB01065 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980684+
1357 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1672 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
224 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
896 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
CHEMBL45 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
DB01065 2440 133 None -1 9 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
10400294 18348 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 258 5 1 3 2.6 Cc1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL127570 18348 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 258 5 1 3 2.6 Cc1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
122188347 122634 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 232 3 1 2 2.0 CCC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612604 122634 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 232 3 1 2 2.0 CCC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
139451780 185352 0 None 5 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 303 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CC1 10.1021/acs.jmedchem.0c00627
CHEMBL4869463 185352 0 None 5 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 303 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CC1 10.1021/acs.jmedchem.0c00627
46935150 15688 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 249 6 1 3 2.0 COc1cccc(O[C@@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223130 15688 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 249 6 1 3 2.0 COc1cccc(O[C@@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
9884406 205882 0 None -3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 341 6 1 3 3.9 COc1ccc2oc(Cc3cccc(F)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL95166 205882 0 None -3 2 Human 9.1 pKi = 9.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 341 6 1 3 3.9 COc1ccc2oc(Cc3cccc(F)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
10361427 112360 0 None 18 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 364 10 1 3 4.9 CCC(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL330969 112360 0 None 18 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 364 10 1 3 4.9 CCC(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
12324 3836 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 591 13 3 4 7.0 O=C(C)NCCc1c(Br)[nH]c2c1cc(cc2)OCCCCCCNC(=O)Oc1cc(ccc1)c1ccccc1 10.1021/acs.jmedchem.8b00893
145966622 3836 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 591 13 3 4 7.0 O=C(C)NCCc1c(Br)[nH]c2c1cc(cc2)OCCCCCCNC(=O)Oc1cc(ccc1)c1ccccc1 10.1021/acs.jmedchem.8b00893
CHEMBL4210086 3836 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 591 13 3 4 7.0 O=C(C)NCCc1c(Br)[nH]c2c1cc(cc2)OCCCCCCNC(=O)Oc1cc(ccc1)c1ccccc1 10.1021/acs.jmedchem.8b00893
10515048 116298 0 None -8 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 253 4 1 1 3.4 CCCC(=O)NCC1Cc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL337882 116298 0 None -8 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 253 4 1 1 3.4 CCCC(=O)NCC1Cc2cccc3cccc1c23 10.1021/jm000922c
46888520 8541 0 None 10 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 538 15 2 4 6.1 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095195 8541 0 None 10 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 538 15 2 4 6.1 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
10199282 116080 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 3 1 2 3.0 COc1ccc2cccc3c2c1CCC3CNC(C)=O 10.1021/jm000922c
CHEMBL336647 116080 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 269 3 1 2 3.0 COc1ccc2cccc3c2c1CCC3CNC(C)=O 10.1021/jm000922c
145982167 166047 0 None -7 3 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 305 4 1 3 2.4 COc1ccc2ccc3c(c2c1)C(CNS(C)(=O)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4280601 166047 0 None -7 3 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 305 4 1 3 2.4 COc1ccc2ccc3c(c2c1)C(CNS(C)(=O)=O)CC3 10.1016/j.ejmech.2017.10.025
145990662 166365 0 None -2 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 312 4 2 2 3.4 CCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4286896 166365 0 None -2 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 312 4 2 2 3.4 CCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137636213 155533 0 None -8 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 273 5 2 3 2.1 CCNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4062947 155533 0 None -8 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 273 5 2 3 2.1 CCNC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
24750192 3842 10 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 10.1021/jm700957j
7777 3842 10 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 10.1021/jm700957j
CHEMBL237236 3842 10 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 10.1021/jm700957j
24750193 88111 1 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 236 6 1 3 1.7 COc1cccc(N(C)CCCNC(C)=O)c1 10.1021/jm700957j
CHEMBL235329 88111 1 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 236 6 1 3 1.7 COc1cccc(N(C)CCCNC(C)=O)c1 10.1021/jm700957j
1357 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1672 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
224 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
896 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
CHEMBL45 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
DB01065 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
139451757 184238 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 311 6 1 5 2.2 CCOc1nc2cc(Cl)c(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4852096 184238 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 311 6 1 5 2.2 CCOc1nc2cc(Cl)c(OC)cc2n1CCNC(C)=O 10.1021/acs.jmedchem.0c00627
1357 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1672 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
224 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
896 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
CHEMBL45 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
DB01065 2440 133 None -1 9 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
53238182 61676 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 339 5 1 3 3.8 CC(=O)NCCC1=C(Cc2ccsc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774520 61676 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 339 5 1 3 3.8 CC(=O)NCCC1=C(Cc2ccsc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
44358274 28725 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 261 2 2 3 1.1 CNC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL138012 28725 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 261 2 2 3 1.1 CNC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
9937825 8765 0 None 12 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 564 17 2 4 6.7 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)CC=C)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1097315 8765 0 None 12 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 564 17 2 4 6.7 C=CCC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)CC=C)c4c3)cc12 10.1016/j.bmc.2010.04.008
49865268 15686 0 None 13 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 249 6 1 3 2.0 COc1cccc(OC(C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223128 15686 0 None 13 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 249 6 1 3 2.0 COc1cccc(OC(C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
44272335 68319 0 None -23 2 Human 9.0 pKi = 9.0 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 7 2 3 3.6 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CCC)N2 10.1016/j.bmcl.2003.12.052
CHEMBL19211 68319 0 None -23 2 Human 9.0 pKi = 9.0 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 7 2 3 3.6 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CCC)N2 10.1016/j.bmcl.2003.12.052
9817636 20460 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 295 4 1 2 3.4 COc1ccc2cccc3c2c1CCC3CNC(=O)C1CC1 10.1021/jm000922c
CHEMBL130876 20460 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 295 4 1 2 3.4 COc1ccc2cccc3c2c1CCC3CNC(=O)C1CC1 10.1021/jm000922c
44272410 67659 0 None -7 2 Human 9.0 pKi = 9.0 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 274 5 2 3 2.9 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(C)=O)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL19128 67659 0 None -7 2 Human 9.0 pKi = 9.0 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 274 5 2 3 2.9 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(C)=O)c2O1 10.1016/j.bmcl.2003.12.052
44389812 62658 0 None 19 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 365 10 1 2 4.9 CCC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL178678 62658 0 None 19 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 365 10 1 2 4.9 CCC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
11581340 121814 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 363 8 1 2 4.6 CC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL359921 121814 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 363 8 1 2 4.6 CC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
20590653 122746 0 None 5 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 389 9 1 2 5.0 O=C(NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2)C1CC1 10.1016/j.bmcl.2005.01.015
CHEMBL361410 122746 0 None 5 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 389 9 1 2 5.0 O=C(NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2)C1CC1 10.1016/j.bmcl.2005.01.015
20590654 129635 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 377 9 1 2 5.0 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL367797 129635 0 None 1 2 Human 9.0 pKi = 9 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 377 9 1 2 5.0 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
44264892 203459 0 None -5 2 Human 9.0 pKi = 9 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 284 5 1 3 3.8 CCC(=O)Nc1ccc(N(C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7832 203459 0 None -5 2 Human 9.0 pKi = 9 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 284 5 1 3 3.8 CCC(=O)Nc1ccc(N(C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
139451799 185247 0 None 3 2 Human 9.0 pKi = 9 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 279 5 1 5 1.9 COc1ccc2nc(SC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4867553 185247 0 None 3 2 Human 9.0 pKi = 9 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 279 5 1 5 1.9 COc1ccc2nc(SC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
145979689 166059 0 None -5 2 Human 9.0 pKi = 9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 314 3 2 2 3.1 CNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4280791 166059 0 None -5 2 Human 9.0 pKi = 9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 314 3 2 2 3.1 CNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145993214 166187 0 None -5 3 Human 9.0 pKi = 9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 285 3 2 3 2.2 CNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4283539 166187 0 None -5 3 Human 9.0 pKi = 9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 285 3 2 3 2.2 CNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
11110447 206044 0 None -4 2 Human 9.0 pKi = 9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 335 6 1 3 4.3 C/C=C/C(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL96104 206044 0 None -4 2 Human 9.0 pKi = 9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 335 6 1 3 4.3 C/C=C/C(=O)NCCc1c(-c2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
9850873 8764 0 None 13 2 Human 9.0 pKi = 9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 564 15 2 4 6.4 O=C(NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C5CC5)c4c3)cc12)C1CC1 10.1016/j.bmc.2010.04.008
CHEMBL1097314 8764 0 None 13 2 Human 9.0 pKi = 9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 564 15 2 4 6.4 O=C(NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C5CC5)c4c3)cc12)C1CC1 10.1016/j.bmc.2010.04.008
10753255 117974 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 251 3 1 1 3.0 O=C(NCC1Cc2cccc3cccc1c23)C1CC1 10.1021/jm000922c
CHEMBL341439 117974 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 251 3 1 1 3.0 O=C(NCC1Cc2cccc3cccc1c23)C1CC1 10.1021/jm000922c
18007985 8613 0 None 10 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 538 14 2 4 6.0 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C5CC5)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095832 8613 0 None 10 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 538 14 2 4 6.0 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C5CC5)c4c3)cc12 10.1016/j.bmc.2010.04.008
44264769 96536 0 None -10 2 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 298 6 1 3 4.2 CCCC(=O)Nc1ccc(N(C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL266549 96536 0 None -10 2 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 298 6 1 3 4.2 CCCC(=O)Nc1ccc(N(C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
139451761 184004 0 None 4 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4848885 184004 0 None 4 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
139451769 185550 0 None 1 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)CC 10.1021/acs.jmedchem.0c00627
CHEMBL4872217 185550 0 None 1 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCNC(=O)CC 10.1021/acs.jmedchem.0c00627
53237950 61674 0 None -13 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 314 5 2 2 3.3 CCNC(=O)NCCC1=C(C(C)C)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774517 61674 0 None -13 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 314 5 2 2 3.3 CCNC(=O)NCCC1=C(C(C)C)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
53238186 61680 0 None -54 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 349 5 1 3 3.6 COc1ccccc1C1=C(CCNC(C)=O)c2c(ccc3c2CCO3)C1 10.1021/jm200221q
CHEMBL1774525 61680 0 None -54 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 349 5 1 3 3.6 COc1ccccc1C1=C(CCNC(C)=O)c2c(ccc3c2CCO3)C1 10.1021/jm200221q
10873443 193544 4 None -1 2 Human 9.0 pKi = 9.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 417 5 1 5 2.4 COc1cc2c(CCNC(C)=O)c(I)n(C)c2cc1[N+](=O)[O-] 10.1021/jm011053+
CHEMBL55084 193544 4 None -1 2 Human 9.0 pKi = 9.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 417 5 1 5 2.4 COc1cc2c(CCNC(C)=O)c(I)n(C)c2cc1[N+](=O)[O-] 10.1021/jm011053+
11536239 76334 1 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 2 2 2.6 COc1ccc2[nH]cc(C(C)(C)CNC(C)=O)c2c1 10.1021/jm0512544
CHEMBL206472 76334 1 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 2 2 2.6 COc1ccc2[nH]cc(C(C)(C)CNC(C)=O)c2c1 10.1021/jm0512544
24763223 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 mins
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1039/C5MD00190K
8289 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 mins
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1039/C5MD00190K
CHEMBL3260987 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 mins
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1039/C5MD00190K
20642483 30422 0 None 2 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 272 3 1 3 1.7 O=C(N[C@H]1CCN(c2cccc3c2CCO3)C1)C1CC1 10.1016/j.bmcl.2003.09.030
CHEMBL139439 30422 0 None 2 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 272 3 1 3 1.7 O=C(N[C@H]1CCN(c2cccc3c2CCO3)C1)C1CC1 10.1016/j.bmcl.2003.09.030
10752506 19771 0 None -5 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 239 2 1 1 3.0 CC(=O)NCC1CCc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL130319 19771 0 None -5 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 239 2 1 1 3.0 CC(=O)NCC1CCc2cccc3cccc1c23 10.1021/jm000922c
85880795 110366 0 None 12 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 319 9 1 3 4.0 CCCCCCOc1ccc2c(c1)C(CCNC(C)=O)CCO2 10.1021/jm401343c
CHEMBL3260984 110366 0 None 12 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 319 9 1 3 4.0 CCCCCCOc1ccc2c(c1)C(CCNC(C)=O)CCO2 10.1021/jm401343c
139451767 184411 0 None 2 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 263 5 1 5 1.2 COc1ccc2nc(OC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4854625 184411 0 None 2 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 263 5 1 5 1.2 COc1ccc2nc(OC)n(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
127041169 136312 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 570 14 2 4 5.7 O=C(NCCc1cccc2ccc(OCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
CHEMBL3741890 136312 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 570 14 2 4 5.7 O=C(NCCc1cccc2ccc(OCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
57781248 183970 0 None -1 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 274 4 2 4 1.9 CC(=O)NCCC1CCc2ccc3nc(CO)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4848381 183970 0 None -1 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 274 4 2 4 1.9 CC(=O)NCCC1CCc2ccc3nc(CO)oc3c21 10.1021/acs.jmedchem.0c01836
11644612 77880 0 None -9 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.4 COc1ccc2c(c1)c(C(C)CNC(C)=O)cn2C 10.1021/jm0512544
CHEMBL210791 77880 0 None -9 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.4 COc1ccc2c(c1)c(C(C)CNC(C)=O)cn2C 10.1021/jm0512544
127041169 136312 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 570 14 2 4 5.7 O=C(NCCc1cccc2ccc(OCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
CHEMBL3741890 136312 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 570 14 2 4 5.7 O=C(NCCc1cccc2ccc(OCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
164946945 189625 1 None -1 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5174929 189625 1 None -1 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
9927219 111817 0 None -25 2 Human 8.9 pKi = 8.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL329263 111817 0 None -25 2 Human 8.9 pKi = 8.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
9927219 111817 0 None -25 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 mins
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.5b00982
CHEMBL329263 111817 0 None -25 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 melatonin receptor expressed in HEK cells after 120 mins
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/acs.jmedchem.5b00982
9927219 111817 0 None -25 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm401343c
CHEMBL329263 111817 0 None -25 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 323 6 1 3 3.7 COc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm401343c
10019103 67138 0 None -5 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 323 5 1 2 3.8 CCCC(=O)NCC1Cc2ccccc2Cc2ccc(OC)cc21 10.1021/jm040768k
CHEMBL189395 67138 0 None -5 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 323 5 1 2 3.8 CCCC(=O)NCC1Cc2ccccc2Cc2ccc(OC)cc21 10.1021/jm040768k
10089253 116571 0 None 12 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 350 9 1 3 4.5 CC(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL339265 116571 0 None 12 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 350 9 1 3 4.5 CC(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
10022570 167971 0 None 13 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 378 10 1 3 5.1 CC(C)C(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL435586 167971 0 None 13 2 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 378 10 1 3 5.1 CC(C)C(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
44353165 116401 0 None -7 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 267 4 1 1 3.8 CCCC(=O)NCC1CCc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL338425 116401 0 None -7 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 267 4 1 1 3.8 CCCC(=O)NCC1CCc2cccc3cccc1c23 10.1021/jm000922c
44272438 69951 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 5 2 3 3.3 CC(C)C(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
CHEMBL19441 69951 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 5 2 3 3.3 CC(C)C(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
52918079 60416 0 None -4 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 261 6 1 4 2.0 CCCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
CHEMBL1760947 60416 0 None -4 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 261 6 1 4 2.0 CCCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
57781208 185029 0 None -5 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 320 4 1 3 4.1 CC(=O)NCCC1CCc2ccc3nc(-c4ccccc4)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4864102 185029 0 None -5 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 320 4 1 3 4.1 CC(=O)NCCC1CCc2ccc3nc(-c4ccccc4)oc3c21 10.1021/acs.jmedchem.0c01836
53238412 61686 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 375 4 1 3 4.8 CC(=O)NCCC1=C(c2csc3ccccc23)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774531 61686 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 375 4 1 3 4.8 CC(=O)NCCC1=C(c2csc3ccccc23)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
10763177 24518 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 393 7 1 4 3.2 CCC(=O)NCCc1c(OC(=O)CBr)ccc2ccc(OC)cc12 10.1021/jm970437q
CHEMBL134416 24518 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 393 7 1 4 3.2 CCC(=O)NCCc1c(OC(=O)CBr)ccc2ccc(OC)cc12 10.1021/jm970437q
10850411 114845 0 None -4 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 281 4 1 2 3.0 COc1ccc2cccc3c2c1C(CNC(=O)C1CC1)C3 10.1021/jm000922c
CHEMBL334962 114845 0 None -4 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 281 4 1 2 3.0 COc1ccc2cccc3c2c1C(CNC(=O)C1CC1)C3 10.1021/jm000922c
20355585 110363 5 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 280 4 2 2 2.8 COc1cc2c(CCNC(C)=O)c(C)[nH]c2cc1Cl 10.1021/jm401343c
CHEMBL3260979 110363 5 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 280 4 2 2 2.8 COc1cc2c(CCNC(C)=O)c(C)[nH]c2cc1Cl 10.1021/jm401343c
10244841 67140 1 None -8 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 309 4 1 2 3.5 CCC(=O)NCC1Cc2ccccc2Cc2ccc(OC)cc21 10.1021/jm040768k
CHEMBL189414 67140 1 None -8 2 Human 8.9 pKi = 8.9 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 309 4 1 2 3.5 CCC(=O)NCC1Cc2ccccc2Cc2ccc(OC)cc21 10.1021/jm040768k
23642306 158515 1 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 6 2 3 2.5 CCC(=O)NCC(CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
CHEMBL4097233 158515 1 None 2 3 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 6 2 3 2.5 CCC(=O)NCC(CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
9870683 8786 0 None 9 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 502 13 2 5 5.2 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4occ(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1097496 8786 0 None 9 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 502 13 2 5 5.2 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4occ(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
52918077 60414 2 None -2 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 1 4 1.2 COc1ccc2ccn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760945 60414 2 None -2 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 1 4 1.2 COc1ccc2ccn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
10244841 67140 1 None -8 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 309 4 1 2 3.5 CCC(=O)NCC1Cc2ccccc2Cc2ccc(OC)cc21 10.1021/jm800974d
CHEMBL189414 67140 1 None -8 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 309 4 1 2 3.5 CCC(=O)NCC1Cc2ccccc2Cc2ccc(OC)cc21 10.1021/jm800974d
53238411 61685 0 None -1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 375 4 1 2 4.9 CC(=O)NCCC1=C(c2ccc(C(C)(C)C)cc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774530 61685 0 None -1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 375 4 1 2 4.9 CC(=O)NCCC1=C(c2ccc(C(C)(C)C)cc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
12004056 173640 0 None 13 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 340 6 3 3 2.0 CC(=O)NCCc1c(Br)[nH]c2ccc(OCCO)cc12 10.1016/j.ejmech.2019.111847
CHEMBL4548591 173640 0 None 13 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 340 6 3 3 2.0 CC(=O)NCCc1c(Br)[nH]c2ccc(OCCO)cc12 10.1016/j.ejmech.2019.111847
44358184 116027 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 246 2 1 3 1.3 CC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL336268 116027 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 246 2 1 3 1.3 CC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
46845151 8563 0 None 38 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 499 12 2 4 6.1 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cc(C(C)C(=O)O)ccc4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095505 8563 0 None 38 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 499 12 2 4 6.1 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cc(C(C)C(=O)O)ccc4c3)cc12 10.1016/j.bmc.2010.04.008
137641357 156525 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.1 CC(=O)NCC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4074273 156525 0 None -3 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.1 CC(=O)NCC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
122188351 122637 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.7 CCC(=O)NCC1CCc2ccccc2N1c1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612608 122637 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.7 CCC(=O)NCC1CCc2ccccc2N1c1ccccc1 10.1021/acs.jmedchem.5b01066
19703015 137359 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 234 4 1 4 1.5 COc1ccc2occ(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3763281 137359 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 234 4 1 4 1.5 COc1ccc2occ(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
11630146 77716 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 246 4 2 2 2.4 COc1ccc2[nH]cc(C(C)CNC(C)=O)c2c1 10.1021/jm0512544
CHEMBL210147 77716 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 246 4 2 2 2.4 COc1ccc2[nH]cc(C(C)CNC(C)=O)c2c1 10.1021/jm0512544
49865204 15659 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(O[C@@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223050 15659 0 None 2 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(O[C@@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
44429442 149678 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 5 2 2 2.6 CCC(=O)NCCc1c[nH]c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL395221 149678 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 5 2 2 2.6 CCC(=O)NCCc1c[nH]c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
44272443 193805 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 6 2 3 3.5 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
CHEMBL553105 193805 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 6 2 3 3.5 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
9858255 206327 0 None -30 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 320 4 1 3 3.4 COc1ccc2c(c1)c(CCNC(C)=O)c1n2Cc2ccccc2-1 10.1021/jm980684+
CHEMBL9772 206327 0 None -30 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 320 4 1 3 3.4 COc1ccc2c(c1)c(CCNC(C)=O)c1n2Cc2ccccc2-1 10.1021/jm980684+
168296374 191910 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
CHEMBL5209359 191910 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
10542922 116079 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 309 5 1 2 3.8 COc1ccc2cccc3c2c1CCC3CCNC(=O)C1CC1 10.1021/jm000922c
CHEMBL336633 116079 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 309 5 1 2 3.8 COc1ccc2cccc3c2c1CCC3CCNC(=O)C1CC1 10.1021/jm000922c
127026427 137146 0 None -3 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3oc(CNC(=O)C4CC4)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3758679 137146 0 None -3 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3oc(CNC(=O)C4CC4)cc3c2c1 10.1016/j.ejmech.2015.12.047
122220128 159116 0 None -5 3 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 309 6 2 3 2.3 COc1ccc2cccc(C(CO)CNC(=O)C(F)F)c2c1 10.1039/C4MD00149D
CHEMBL4104020 159116 0 None -5 3 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 309 6 2 3 2.3 COc1ccc2cccc(C(CO)CNC(=O)C(F)F)c2c1 10.1039/C4MD00149D
10637638 20386 0 None 4 2 Human 8.0 pKi = 8 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 295 5 1 2 3.4 COc1ccc2cccc3c2c1C(CCNC(=O)C1CC1)C3 10.1021/jm000922c
CHEMBL130813 20386 0 None 4 2 Human 8.0 pKi = 8 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 295 5 1 2 3.4 COc1ccc2cccc3c2c1C(CCNC(=O)C1CC1)C3 10.1021/jm000922c
127026424 137154 0 None -5 2 Human 8.0 pKi = 8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 283 4 1 3 3.3 COc1ccc2ccc3oc(CCNC(C)=O)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3758720 137154 0 None -5 2 Human 8.0 pKi = 8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 283 4 1 3 3.3 COc1ccc2ccc3oc(CCNC(C)=O)cc3c2c1 10.1016/j.ejmech.2015.12.047
44394415 123875 0 None 1 2 Human 8.0 pKi = 8 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 389 10 1 2 6.0 CCCC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL363947 123875 0 None 1 2 Human 8.0 pKi = 8 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 389 10 1 2 6.0 CCCC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
44429449 86921 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 324 4 1 3 2.6 COc1cc(Br)c2c(c1)c(CCNC(C)=O)cn2C 10.1016/j.bmc.2007.04.013
CHEMBL233309 86921 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 324 4 1 3 2.6 COc1cc(Br)c2c(c1)c(CCNC(C)=O)cn2C 10.1016/j.bmc.2007.04.013
11536939 76746 0 None -12 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 314 6 1 3 3.5 CCCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCC1 10.1021/jm0512544
CHEMBL207625 76746 0 None -12 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 314 6 1 3 3.5 CCCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCC1 10.1021/jm0512544
44264818 203504 0 None -91 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 6 1 2 4.0 CCCC(=O)Nc1ccc(Cc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7867 203504 0 None -91 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 6 1 2 4.0 CCCC(=O)Nc1ccc(Cc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
44359437 29671 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 273 5 2 3 2.1 COc1ccc2cccc(C(CO)CNC(C)=O)c2c1 10.1039/C4MD00149D
CHEMBL138807 29671 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 273 5 2 3 2.1 COc1ccc2cccc(C(CO)CNC(C)=O)c2c1 10.1039/C4MD00149D
10526493 203573 0 None -1 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 427 8 1 3 3.7 CCC(=O)NCCc1c(OCCI)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
CHEMBL79224 203573 0 None -1 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 427 8 1 3 3.7 CCC(=O)NCCc1c(OCCI)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
24750188 148700 0 None -114 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 314 7 1 4 3.0 COc1ccc(N(CCNC(C)=O)c2cccc(OC)c2)cc1 10.1021/jm700957j
CHEMBL394430 148700 0 None -114 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 314 7 1 4 3.0 COc1ccc(N(CCNC(C)=O)c2cccc(OC)c2)cc1 10.1021/jm700957j
16105169 174095 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 345 3 1 3 3.3 CC(=O)NCCc1c2n(c3ccccc13)CC1Cc3ccccc3N1C2 10.1016/j.bmc.2009.04.068
CHEMBL455909 174095 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 345 3 1 3 3.3 CC(=O)NCCc1c2n(c3ccccc13)CC1Cc3ccccc3N1C2 10.1016/j.bmc.2009.04.068
45268309 194587 0 None -4 2 Human 6.0 pKi = 6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 303 7 2 3 2.3 CCN(C)Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1016/j.bmc.2009.04.068
CHEMBL561928 194587 0 None -4 2 Human 6.0 pKi = 6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 303 7 2 3 2.3 CCN(C)Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1016/j.bmc.2009.04.068
16105169 174095 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 345 3 1 3 3.3 CC(=O)NCCc1c2n(c3ccccc13)CC1Cc3ccccc3N1C2 10.1016/j.bmc.2008.07.012
CHEMBL455909 174095 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 345 3 1 3 3.3 CC(=O)NCCc1c2n(c3ccccc13)CC1Cc3ccccc3N1C2 10.1016/j.bmc.2008.07.012
25210130 69 0 None -91 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
7782 69 0 None -91 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
CHEMBL514415 69 0 None -91 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
1358 124 35 None -870 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm048956y
3976006 124 35 None -870 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm048956y
CHEMBL285718 124 35 None -870 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm048956y
54584155 60417 0 None -2 2 Human 5.0 pKi = 5.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 366 8 1 5 2.8 COc1ccc2c(CN(C)Cc3ccccc3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760949 60417 0 None -2 2 Human 5.0 pKi = 5.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 366 8 1 5 2.8 COc1ccc2c(CN(C)Cc3ccccc3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
49865148 15640 2 None -2 2 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1ccccc1OC(C)CNC(C)=O 10.1016/j.bmc.2010.06.100
CHEMBL1222984 15640 2 None -2 2 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1ccccc1OC(C)CNC(C)=O 10.1016/j.bmc.2010.06.100
44394478 65942 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 404 8 1 3 5.3 CC(C)C(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
CHEMBL184762 65942 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 404 8 1 3 5.3 CC(C)C(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
44264849 203651 0 None -19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 298 5 1 3 4.1 COc1cccc(N(C)c2ccc(NC(=O)C(C)C)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL7990 203651 0 None -19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 298 5 1 3 4.1 COc1cccc(N(C)c2ccc(NC(=O)C(C)C)cc2)c1 10.1016/j.bmcl.2003.11.030
10956792 101328 7 None -1 2 Human 6.0 pKi = 6.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 277 5 2 4 1.8 COc1ccc2[nH]cc(CCNC(C)=O)c2c1[N+](=O)[O-] 10.1021/jm011053+
CHEMBL300195 101328 7 None -1 2 Human 6.0 pKi = 6.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 277 5 2 4 1.8 COc1ccc2[nH]cc(CCNC(C)=O)c2c1[N+](=O)[O-] 10.1021/jm011053+
25210135 174342 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 378 6 3 4 3.0 COc1ccc2[nH]c(CN3CCc4ccc(N)cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL456505 174342 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 378 6 3 4 3.0 COc1ccc2[nH]c(CN3CCc4ccc(N)cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
25210135 174342 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 378 6 3 4 3.0 COc1ccc2[nH]c(CN3CCc4ccc(N)cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL456505 174342 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 378 6 3 4 3.0 COc1ccc2[nH]c(CN3CCc4ccc(N)cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
45268310 194878 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 419 7 2 3 4.5 COc1ccc2[nH]c(CN(C)c3ccc(C(F)(F)F)cc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
CHEMBL563847 194878 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 419 7 2 3 4.5 COc1ccc2[nH]c(CN(C)c3ccc(C(F)(F)F)cc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
46935149 15660 2 None 2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SC(C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223051 15660 2 None 2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SC(C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
44394508 65799 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 404 9 1 3 5.5 CCCC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
CHEMBL184144 65799 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 404 9 1 3 5.5 CCCC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
10831675 21565 0 None -6 2 Human 8.0 pKi = 8.0 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 349 7 1 4 3.1 CCC(=O)NCCc1c(OC(=O)CCl)ccc2ccc(OC)cc12 10.1021/jm970437q
CHEMBL131919 21565 0 None -6 2 Human 8.0 pKi = 8.0 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 349 7 1 4 3.1 CCC(=O)NCCc1c(OC(=O)CCl)ccc2ccc(OC)cc12 10.1021/jm970437q
1346 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1016/j.ejmech.2019.111847
1858 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1016/j.ejmech.2019.111847
CHEMBL34730 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1016/j.ejmech.2019.111847
1346 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1021/jm401343c
1858 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1021/jm401343c
CHEMBL34730 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1021/jm401343c
11587169 76949 0 None -8 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 4 1 3 2.6 COc1ccc2c(c1)c(C(C)(C)CNC(C)=O)cn2C 10.1021/jm0512544
CHEMBL208307 76949 0 None -8 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 4 1 3 2.6 COc1ccc2c(c1)c(C(C)(C)CNC(C)=O)cn2C 10.1021/jm0512544
127041170 136153 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 584 15 2 4 6.1 O=C(NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
CHEMBL3740377 136153 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 584 15 2 4 6.1 O=C(NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
45268303 195060 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 301 4 1 4 1.8 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCN(C)C1 10.1016/j.bmc.2009.04.068
CHEMBL565176 195060 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 301 4 1 4 1.8 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCN(C)C1 10.1016/j.bmc.2009.04.068
44272424 68718 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 289 4 3 3 2.5 CNC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
CHEMBL19237 68718 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 289 4 3 3 2.5 CNC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
11666721 64644 0 None -18 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 1 4 2.7 CNC(=O)CCc1c(-c2ccccc2)nc2ccc(OC)cn12 10.1016/j.ejmech.2011.06.030
CHEMBL1823016 64644 0 None -18 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 1 4 2.7 CNC(=O)CCc1c(-c2ccccc2)nc2ccc(OC)cn12 10.1016/j.ejmech.2011.06.030
45268310 194878 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 419 7 2 3 4.5 COc1ccc2[nH]c(CN(C)c3ccc(C(F)(F)F)cc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
CHEMBL563847 194878 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 419 7 2 3 4.5 COc1ccc2[nH]c(CN(C)c3ccc(C(F)(F)F)cc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
1362 3370 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9870523 3370 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL429392 3370 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
11403195 123149 1 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 278 3 1 2 3.4 CC(=O)NCCN1c2ccccc2C=Cc2ccccc21 10.1021/jm040768k
CHEMBL362133 123149 1 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 278 3 1 2 3.4 CC(=O)NCCN1c2ccccc2C=Cc2ccccc21 10.1021/jm040768k
90666309 108885 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 7 2 3 4.2 COc1ccc2[nH]c(CN3Cc4ccccc4C3)c(CCNC(=O)C3CCC3)c2c1 10.1039/C1MD00149C
CHEMBL3219330 108885 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 7 2 3 4.2 COc1ccc2[nH]c(CN3Cc4ccccc4C3)c(CCNC(=O)C3CCC3)c2c1 10.1039/C1MD00149C
1362 3370 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9870523 3370 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL429392 3370 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
25210130 69 0 None -91 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
7782 69 0 None -91 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
CHEMBL514415 69 0 None -91 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
16743124 91763 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 282 5 1 2 3.0 O=C(NCCCc1cn2c3c(cccc13)CCC2)C1CC1 10.1016/j.ejmech.2007.01.005
CHEMBL242573 91763 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 282 5 1 2 3.0 O=C(NCCCc1cn2c3c(cccc13)CCC2)C1CC1 10.1016/j.ejmech.2007.01.005
162661094 180851 2 None -10 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1nncc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
CHEMBL4764211 180851 2 None -10 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1nncc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
12436516 15665 6 None -2 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 179 4 1 2 1.2 CC(=O)NCCOc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223056 15665 6 None -2 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 179 4 1 2 1.2 CC(=O)NCCOc1ccccc1 10.1016/j.bmc.2010.06.100
49865377 15743 0 None 1 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SC[C@@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223280 15743 0 None 1 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SC[C@@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
10664333 206432 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 332 4 1 2 4.3 CCC(=O)NCCc1c2n(c3ccccc13)CCCc1ccccc1-2 10.1021/jm980684+
CHEMBL9838 206432 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 332 4 1 2 4.3 CCC(=O)NCCc1c2n(c3ccccc13)CCCc1ccccc1-2 10.1021/jm980684+
122188227 122616 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 233 3 3 2 1.7 CCNC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612458 122616 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 233 3 3 2 1.7 CCNC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
22718579 16330 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 5 1 3 3.0 CC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL123690 16330 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 5 1 3 3.0 CC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
11543959 76756 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 6 2 2 3.5 CCCC(=O)NCC1(c2c[nH]c3ccc(OC)cc23)CCC1 10.1021/jm0512544
CHEMBL207676 76756 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 6 2 2 3.5 CCCC(=O)NCC1(c2c[nH]c3ccc(OC)cc23)CCC1 10.1021/jm0512544
11791741 206360 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 344 4 1 2 4.3 O=C(NCCc1c2n(c3ccccc13)CCCc1ccccc1-2)C1CC1 10.1021/jm980684+
CHEMBL9791 206360 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 344 4 1 2 4.3 O=C(NCCc1c2n(c3ccccc13)CCCc1ccccc1-2)C1CC1 10.1021/jm980684+
46885228 7609 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 341 10 1 3 4.1 CCCC(=O)NCCCc1cc(OC)ccc1OCc1ccccc1 10.1016/j.bmcl.2010.02.084
CHEMBL1088825 7609 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 341 10 1 3 4.1 CCCC(=O)NCCCc1cc(OC)ccc1OCc1ccccc1 10.1016/j.bmcl.2010.02.084
22718619 16580 0 None -7 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 7 1 3 3.8 CCCC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL124445 16580 0 None -7 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 7 1 3 3.8 CCCC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
44264844 203144 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 296 5 1 3 3.8 COc1cccc(N(C)c2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL7567 203144 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 296 5 1 3 3.8 COc1cccc(N(C)c2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
127041170 136153 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 584 15 2 4 6.1 O=C(NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
CHEMBL3740377 136153 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 584 15 2 4 6.1 O=C(NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CCNC(=O)C(F)F)c4c3)cc12)C(F)F 10.1039/C5MD00190K
145964105 163655 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 475 12 2 5 4.9 CC(=O)NCCN(C)c1cccc(OCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4211018 163655 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 475 12 2 5 4.9 CC(=O)NCCN(C)c1cccc(OCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
11068422 206099 0 None -7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 361 6 1 4 4.7 COc1ccc2oc(-c3ccccc3)c(CCNC(=O)c3ccco3)c2c1 10.1021/jm0005252
CHEMBL96420 206099 0 None -7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 361 6 1 4 4.7 COc1ccc2oc(-c3ccccc3)c(CCNC(=O)c3ccco3)c2c1 10.1021/jm0005252
127038225 137448 0 None -13 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 338 5 1 4 3.8 COc1ccc2oc(-c3c(C)cccc3C)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3764421 137448 0 None -13 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 338 5 1 4 3.8 COc1ccc2oc(-c3c(C)cccc3C)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
25210134 189022 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 315 6 2 3 2.5 COc1ccc2[nH]c(CN3CCCC3)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL514904 189022 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 315 6 2 3 2.5 COc1ccc2[nH]c(CN3CCCC3)c(CCNC(C)=O)c2c1 10.1021/jm800974d
49865317 15703 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 265 6 1 3 2.7 COc1cccc(S[C@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223191 15703 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 265 6 1 3 2.7 COc1cccc(S[C@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
10544425 206586 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 330 4 1 2 4.1 O=C(NCCc1c2n(c3ccccc13)Cc1ccccc1-2)C1CCC1 10.1021/jm980684+
CHEMBL9934 206586 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 330 4 1 2 4.1 O=C(NCCc1c2n(c3ccccc13)Cc1ccccc1-2)C1CCC1 10.1021/jm980684+
16094578 82845 1 None -8 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 251 4 1 1 3.4 CC(=O)NC/C(=C\c1ccccc1)c1ccccc1 10.1021/jm060850a
CHEMBL218808 82845 1 None -8 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 251 4 1 1 3.4 CC(=O)NC/C(=C\c1ccccc1)c1ccccc1 10.1021/jm060850a
12436514 15736 6 None -3 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)NC(C)COc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223273 15736 6 None -3 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)NC(C)COc1ccccc1 10.1016/j.bmc.2010.06.100
49865376 15742 2 None -9 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SCC(C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223279 15742 2 None -9 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SCC(C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
25210134 189022 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 315 6 2 3 2.5 COc1ccc2[nH]c(CN3CCCC3)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL514904 189022 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 315 6 2 3 2.5 COc1ccc2[nH]c(CN3CCCC3)c(CCNC(C)=O)c2c1 10.1021/jm800974d
46865422 86629 0 None -575 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326199 86629 0 None -575 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
54586061 60420 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 441 7 1 6 3.2 COc1ccc2c(CN3CCN(c4cccc(Cl)c4)CC3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760952 60420 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 441 7 1 6 3.2 COc1ccc2c(CN3CCN(c4cccc(Cl)c4)CC3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
122188238 122626 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.1 CC(=O)NC[C@@H]1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612470 122626 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.1 CC(=O)NC[C@@H]1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
10656443 206624 2 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 218 3 2 2 1.8 COc1cccc2[nH]c(CNC(C)=O)cc12 10.1021/jm001125h
CHEMBL99534 206624 2 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 218 3 2 2 1.8 COc1cccc2[nH]c(CNC(C)=O)cc12 10.1021/jm001125h
10656443 206624 2 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 218 3 2 2 1.8 COc1cccc2[nH]c(CNC(C)=O)cc12 10.1021/jm970721h
CHEMBL99534 206624 2 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 218 3 2 2 1.8 COc1cccc2[nH]c(CNC(C)=O)cc12 10.1021/jm970721h
137660180 158564 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 270 5 1 3 2.3 COc1cnc2cccc(CCNC(=O)C3CC3)c2c1 10.1016/j.ejmech.2016.12.013
CHEMBL4097817 158564 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 270 5 1 3 2.3 COc1cnc2cccc(CCNC(=O)C3CC3)c2c1 10.1016/j.ejmech.2016.12.013
44579164 181538 0 None -14 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 406 7 2 4 4.8 CCOC(=O)Nc1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
CHEMBL478218 181538 0 None -14 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 406 7 2 4 4.8 CCOC(=O)Nc1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
12985494 190025 0 None -239 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 363 7 2 3 4.1 CCC(=O)NCCc1cc(-c2cccc(CO)c2)cc2ccc(OC)cc12 10.1016/j.bmc.2008.08.052
CHEMBL518113 190025 0 None -239 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 363 7 2 3 4.1 CCC(=O)NCCc1cc(-c2cccc(CO)c2)cc2ccc(OC)cc12 10.1016/j.bmc.2008.08.052
24750190 89441 2 None -32 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 254 5 1 2 3.0 CC(=O)NCCN(c1ccccc1)c1ccccc1 10.1021/jm700957j
CHEMBL237840 89441 2 None -32 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 254 5 1 2 3.0 CC(=O)NCCN(c1ccccc1)c1ccccc1 10.1021/jm700957j
44429455 87306 0 None -2 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 322 5 1 3 3.5 COc1cc(-c2ccccc2)c2c(c1)c(CCNC(C)=O)cn2C 10.1016/j.bmc.2007.04.013
CHEMBL233740 87306 0 None -2 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 322 5 1 3 3.5 COc1cc(-c2ccccc2)c2c(c1)c(CCNC(C)=O)cn2C 10.1016/j.bmc.2007.04.013
12985492 181239 0 None -177 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 459 6 1 2 5.1 COc1ccc2cc(-c3cccc(CI)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL477833 181239 0 None -177 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 459 6 1 2 5.1 COc1ccc2cc(-c3cccc(CI)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
46885283 8156 0 None -48 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 237 6 1 3 1.8 COc1ccc(OC)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1092400 8156 0 None -48 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 237 6 1 3 1.8 COc1ccc(OC)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
10428383 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm001125h
7783 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm001125h
CHEMBL33185 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm001125h
10903368 206354 0 None -4 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 322 6 1 3 3.7 CCC(=O)NCc1cc2ccc(OC)cc2n1Cc1ccccc1 10.1021/jm001125h
CHEMBL97885 206354 0 None -4 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 322 6 1 3 3.7 CCC(=O)NCc1cc2ccc(OC)cc2n1Cc1ccccc1 10.1021/jm001125h
45267465 193089 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 365 8 2 3 3.5 COc1ccc2[nH]c(CN(C)Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
CHEMBL538129 193089 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 365 8 2 3 3.5 COc1ccc2[nH]c(CN(C)Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
24750195 88112 0 None -24 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 298 6 0 3 3.3 COc1cccc(N(CCN(C)C(C)=O)c2ccccc2)c1 10.1021/jm700957j
CHEMBL235334 88112 0 None -24 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 298 6 0 3 3.3 COc1cccc(N(CCN(C)C(C)=O)c2ccccc2)c1 10.1021/jm700957j
10428383 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm048956y
7783 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm048956y
CHEMBL33185 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm048956y
44429452 86923 0 None -4 2 Human 4.9 pKi = 4.9 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 308 5 2 2 3.5 COc1cc(-c2ccccc2)c2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.04.013
CHEMBL233311 86923 0 None -4 2 Human 4.9 pKi = 4.9 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 308 5 2 2 3.5 COc1cc(-c2ccccc2)c2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.04.013
44358087 115900 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 3 1 3 2.0 CC(C)C(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL336024 115900 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 3 1 3 2.0 CC(C)C(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
10428383 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human MT1 receptorAntagonist activity at human MT1 receptor
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm401343c
7783 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human MT1 receptorAntagonist activity at human MT1 receptor
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm401343c
CHEMBL33185 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human MT1 receptorAntagonist activity at human MT1 receptor
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm401343c
10428383 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm800974d
7783 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm800974d
CHEMBL33185 3838 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm800974d
139451766 183855 0 None -8 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 325 7 1 5 2.6 CCOc1nc2cc(Cl)c(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4846505 183855 0 None -8 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 325 7 1 5 2.6 CCOc1nc2cc(Cl)c(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
122188225 122614 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 218 3 2 2 1.9 CCC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612456 122614 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 218 3 2 2 1.9 CCC(=O)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
122193492 123411 0 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 261 4 1 4 1.5 COc1ccc2oc(=O)cc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2015.09.003
CHEMBL3628489 123411 0 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometryDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 expressed in CHO cell membranes incubated for 60 mins by liquid scintillation spectrometry
ChEMBL 261 4 1 4 1.5 COc1ccc2oc(=O)cc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2015.09.003
53238410 61684 0 None -1174 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 361 5 1 2 4.7 CC(=O)NCCC1=C(c2cccc(C(C)C)c2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774529 61684 0 None -1174 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 361 5 1 2 4.7 CC(=O)NCCC1=C(c2cccc(C(C)C)c2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
22718610 16693 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 308 6 1 3 4.0 CCC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL125033 16693 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 308 6 1 3 4.0 CCC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
22718602 96084 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 6 1 3 3.1 CCc1nc2cccc(CCCNC(=O)C(C)C)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL262890 96084 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 6 1 3 3.1 CCc1nc2cccc(CCCNC(=O)C(C)C)c2o1 10.1016/j.bmcl.2004.04.082
24750189 89036 0 None -1174 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 334 6 1 3 4.1 COc1cccc(N(CCNC(C)=O)c2ccc3ccccc3c2)c1 10.1021/jm700957j
CHEMBL237234 89036 0 None -1174 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 334 6 1 3 4.1 COc1cccc(N(CCNC(C)=O)c2ccc3ccccc3c2)c1 10.1021/jm700957j
122188232 122620 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 353 6 2 3 3.3 CCNC(=O)NCC1CCc2c(OC)cccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612463 122620 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 353 6 2 3 3.3 CCNC(=O)NCC1CCc2c(OC)cccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
44581851 174629 0 None -1202 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 333 6 1 2 4.5 COc1cccc(C(CCNC(C)=O)c2ccc3ccccc3c2)c1 10.1021/jm800974d
CHEMBL457128 174629 0 None -1202 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 333 6 1 2 4.5 COc1cccc(C(CCNC(C)=O)c2ccc3ccccc3c2)c1 10.1021/jm800974d
10610443 206556 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 246 5 2 2 2.2 CCC(=O)NCCc1cc2c(OC)cccc2[nH]1 10.1021/jm001125h
CHEMBL99084 206556 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 246 5 2 2 2.2 CCC(=O)NCCc1cc2c(OC)cccc2[nH]1 10.1021/jm001125h
10610443 206556 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 246 5 2 2 2.2 CCC(=O)NCCc1cc2c(OC)cccc2[nH]1 10.1021/jm970721h
CHEMBL99084 206556 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 246 5 2 2 2.2 CCC(=O)NCCc1cc2c(OC)cccc2[nH]1 10.1021/jm970721h
46865422 86629 0 None -575 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1039/C1MD00149C
CHEMBL2326199 86629 0 None -575 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1039/C1MD00149C
46865422 86629 0 None -575 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1016/j.ejmech.2016.01.008
CHEMBL2326199 86629 0 None -575 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 357 10 1 4 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1cccc(OC)c1 10.1016/j.ejmech.2016.01.008
44579259 186521 0 None -331 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 347 6 1 3 4.0 COc1ccc2cc(-c3cccc(C=O)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL491604 186521 0 None -331 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 347 6 1 3 4.0 COc1ccc2cc(-c3cccc(C=O)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
12436515 15641 2 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)NCC(C)Oc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1222985 15641 2 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)NCC(C)Oc1ccccc1 10.1016/j.bmc.2010.06.100
10427851 181241 0 None -407 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 348 6 2 3 3.7 COc1ccc2cc(-c3cccc(CN)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL477834 181241 0 None -407 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 348 6 2 3 3.7 COc1ccc2cc(-c3cccc(CN)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
86273227 120790 0 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 242 4 2 2 1.5 C#CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580907 120790 0 None -3 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 242 4 2 2 1.5 C#CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
44429450 86922 0 None -6 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 338 5 1 3 3.0 CCC(=O)NCCc1cn(C)c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL233310 86922 0 None -6 2 Human 7.9 pKi = 7.9 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 338 5 1 3 3.0 CCC(=O)NCCc1cn(C)c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
11824364 112047 0 None -42 2 Human 7.8 pKi = 7.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1ccc2oc(Cc3ccccc3OC)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL329960 112047 0 None -42 2 Human 7.8 pKi = 7.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1ccc2oc(Cc3ccccc3OC)c(CCNC(C)=O)c2c1 10.1021/jm0005252
56671857 64107 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 384 13 1 4 4.3 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2ccccc2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813324 64107 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 384 13 1 4 4.3 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2ccccc2)c1 10.1016/j.bmc.2011.06.063
10617720 206074 0 None -56 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 6 1 3 4.1 CCOc1ccc2c(c1)c(CCNC(=O)CC)c1n2Cc2ccccc2-1 10.1021/jm980684+
CHEMBL9630 206074 0 None -56 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 6 1 3 4.1 CCOc1ccc2c(c1)c(CCNC(=O)CC)c1n2Cc2ccccc2-1 10.1021/jm980684+
3956219 101064 11 None -2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 277 5 2 4 1.8 COc1cc2c(CCNC(C)=O)c[nH]c2cc1[N+](=O)[O-] 10.1021/jm011053+
CHEMBL298335 101064 11 None -2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 277 5 2 4 1.8 COc1cc2c(CCNC(C)=O)c[nH]c2cc1[N+](=O)[O-] 10.1021/jm011053+
127027022 137271 0 None -19 3 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 314 4 2 3 3.6 CCNC(=S)NCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
CHEMBL3759677 137271 0 None -19 3 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 314 4 2 3 3.6 CCNC(=S)NCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
25210132 170300 0 None -9 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 7 2 3 4.2 COc1ccc2[nH]c(CN3CCc4ccccc43)c(CCNC(=O)C3CCC3)c2c1 10.1021/jm800974d
CHEMBL445427 170300 0 None -9 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 7 2 3 4.2 COc1ccc2[nH]c(CN3CCc4ccccc43)c(CCNC(=O)C3CCC3)c2c1 10.1021/jm800974d
10829695 118687 0 None -21 2 Human 6.9 pKi = 6.9 Binding
Binding Affinity (pKi) towards Melatonin receptor type 1ABinding Affinity (pKi) towards Melatonin receptor type 1A
ChEMBL 322 6 1 3 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1ccccc1 10.1021/jm020982d
CHEMBL34327 118687 0 None -21 2 Human 6.9 pKi = 6.9 Binding
Binding Affinity (pKi) towards Melatonin receptor type 1ABinding Affinity (pKi) towards Melatonin receptor type 1A
ChEMBL 322 6 1 3 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1ccccc1 10.1021/jm020982d
10829695 118687 0 None -21 2 Human 6.9 pKi = 6.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 322 6 1 3 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1ccccc1 10.1021/jm048956y
CHEMBL34327 118687 0 None -21 2 Human 6.9 pKi = 6.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 322 6 1 3 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1ccccc1 10.1021/jm048956y
25210132 170300 0 None -9 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 7 2 3 4.2 COc1ccc2[nH]c(CN3CCc4ccccc43)c(CCNC(=O)C3CCC3)c2c1 10.1021/jm800974d
CHEMBL445427 170300 0 None -9 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 7 2 3 4.2 COc1ccc2[nH]c(CN3CCc4ccccc43)c(CCNC(=O)C3CCC3)c2c1 10.1021/jm800974d
22718585 16314 0 None -9 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 6 1 3 3.4 CCC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL123634 16314 0 None -9 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 6 1 3 3.4 CCC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
46884599 8319 0 None -13 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 343 9 1 4 3.4 COc1cccc(COc2ccc(CCCNC(C)=O)cc2OC)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1093457 8319 0 None -13 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 343 9 1 4 3.4 COc1cccc(COc2ccc(CCCNC(C)=O)cc2OC)c1 10.1016/j.bmcl.2010.02.084
25209860 188386 0 None -10 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.8 COc1ccc2[nH]c(CN3c4ccccc4CC3C)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL508552 188386 0 None -10 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.8 COc1ccc2[nH]c(CN3c4ccccc4CC3C)c(CCNC(C)=O)c2c1 10.1021/jm800974d
168274836 189544 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5173623 189544 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
162647716 179297 0 None -3 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 259 5 1 4 1.7 CCC(=O)NCCc1nncc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
CHEMBL4745789 179297 0 None -3 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 259 5 1 4 1.7 CCC(=O)NCCc1nncc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
10853020 97701 0 None -15 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 318 4 1 2 3.9 CCC(=O)NCCc1c2n(c3ccccc13)CCc1ccccc1-2 10.1021/jm980684+
CHEMBL273897 97701 0 None -15 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 318 4 1 2 3.9 CCC(=O)NCCc1c2n(c3ccccc13)CCc1ccccc1-2 10.1021/jm980684+
25209860 188386 0 None -10 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.8 COc1ccc2[nH]c(CN3c4ccccc4CC3C)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL508552 188386 0 None -10 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.8 COc1ccc2[nH]c(CN3c4ccccc4CC3C)c(CCNC(C)=O)c2c1 10.1021/jm800974d
11536746 138908 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 4 1 3 3.1 COc1ccc2c(c1)c(C1(CNC(C)=O)CCCC1)cn2C 10.1021/jm0512544
CHEMBL379403 138908 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 4 1 3 3.1 COc1ccc2c(c1)c(C1(CNC(C)=O)CCCC1)cn2C 10.1021/jm0512544
44241666 194412 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 351 7 2 3 3.5 COc1ccc2[nH]c(CN(C)c3ccccc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
CHEMBL560865 194412 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 351 7 2 3 3.5 COc1ccc2[nH]c(CN(C)c3ccccc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
44429445 87090 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 5 1 3 2.6 CCC(=O)NCCc1cn(C)c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL233516 87090 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 5 1 3 2.6 CCC(=O)NCCc1cn(C)c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
12985496 181739 0 None -31 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 389 7 2 3 4.5 COc1ccc2cc(-c3cccc(CO)c3)cc(CCNC(=O)C3CCC3)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL478438 181739 0 None -31 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 389 7 2 3 4.5 COc1ccc2cc(-c3cccc(CO)c3)cc(CCNC(=O)C3CCC3)c2c1 10.1016/j.bmc.2008.08.052
44412079 165693 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 4 2 3 2.8 CCC(=O)NCC1(c2cn(C)c3ccc(O)cc23)CCC1 10.1021/jm0512544
CHEMBL426861 165693 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 4 2 3 2.8 CCC(=O)NCC1(c2cn(C)c3ccc(O)cc23)CCC1 10.1021/jm0512544
11098363 168539 1 None -14 2 Human 6.8 pKi = 6.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 293 5 1 2 3.7 CC(=O)NCCc1c(Cc2ccccc2)oc2ccccc12 10.1021/jm0005252
CHEMBL440144 168539 1 None -14 2 Human 6.8 pKi = 6.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 293 5 1 2 3.7 CC(=O)NCCc1c(Cc2ccccc2)oc2ccccc12 10.1021/jm0005252
127025786 137311 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 312 5 2 3 3.5 CCNC(=O)NCCc1coc2ccc3ccc(OC)cc3c12 10.1016/j.ejmech.2015.12.047
CHEMBL3760044 137311 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 312 5 2 3 3.5 CCNC(=O)NCCc1coc2ccc3ccc(OC)cc3c12 10.1016/j.ejmech.2015.12.047
127025782 137193 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 297 4 1 3 3.9 COc1ccc2ccc3occ(CNC(=O)C(C)C)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759054 137193 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 297 4 1 3 3.9 COc1ccc2ccc3occ(CNC(=O)C(C)C)c3c2c1 10.1016/j.ejmech.2015.12.047
122162 2345 67 None -18 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm401343c
1363 2345 67 None -18 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm401343c
CHEMBL286615 2345 67 None -18 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm401343c
54581170 60424 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 359 4 1 4 1.8 COc1ccc2c(I)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760956 60424 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 359 4 1 4 1.8 COc1ccc2c(I)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
137660726 158773 0 None -15 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 322 6 1 5 1.6 CCS(=O)(=O)NC(=O)CCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4100108 158773 0 None -15 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 322 6 1 5 1.6 CCS(=O)(=O)NC(=O)CCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
18522267 65978 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 377 11 1 2 5.8 CCCC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL184990 65978 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 377 11 1 2 5.8 CCCC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
44394394 122182 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 387 9 1 2 5.6 O=C(NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12)C1CC1 10.1016/j.bmcl.2004.07.055
CHEMBL360428 122182 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 387 9 1 2 5.6 O=C(NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12)C1CC1 10.1016/j.bmcl.2004.07.055
145971624 164050 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 517 15 2 5 6.0 CCC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4215980 164050 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 517 15 2 5 6.0 CCC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
10849065 137 8 None 4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1345 137 8 None 4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
CHEMBL126809 137 8 None 4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
24750191 88110 0 None -85 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 332 5 1 2 3.7 CC(=O)NCCN(c1ccccc1)c1cccc(Br)c1 10.1021/jm700957j
CHEMBL235328 88110 0 None -85 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 332 5 1 2 3.7 CC(=O)NCCN(c1ccccc1)c1cccc(Br)c1 10.1021/jm700957j
11392720 66701 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 309 4 1 2 3.5 COc1ccc2c(c1)C(CCNC(C)=O)Cc1ccccc1C2 10.1021/jm040768k
CHEMBL187160 66701 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 309 4 1 2 3.5 COc1ccc2c(c1)C(CCNC(C)=O)Cc1ccccc1C2 10.1021/jm040768k
10513752 108001 3 None -1 2 Human 4.8 pKi = 4.8 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2[nH]c(CCNC(C)=O)cc2c1 10.1021/jm001125h
CHEMBL319970 108001 3 None -1 2 Human 4.8 pKi = 4.8 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2[nH]c(CCNC(C)=O)cc2c1 10.1021/jm001125h
10513752 108001 3 None -1 2 Human 4.8 pKi = 4.8 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2[nH]c(CCNC(C)=O)cc2c1 10.1021/jm970721h
CHEMBL319970 108001 3 None -1 2 Human 4.8 pKi = 4.8 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2[nH]c(CCNC(C)=O)cc2c1 10.1021/jm970721h
22718571 16644 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 8 1 3 3.6 CCCC(=O)NCCCc1cccc2nc(CCC)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL124782 16644 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 8 1 3 3.6 CCCC(=O)NCCCc1cccc2nc(CCC)oc12 10.1016/j.bmcl.2004.04.082
121231413 3834 1 None -16982 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2c(N1Cc1ccccc1)cccc2OC 10.1021/acs.jmedchem.5b01066
9226 3834 1 None -16982 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2c(N1Cc1ccccc1)cccc2OC 10.1021/acs.jmedchem.5b01066
CHEMBL3612464 3834 1 None -16982 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2c(N1Cc1ccccc1)cccc2OC 10.1021/acs.jmedchem.5b01066
86273229 120792 1 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 244 5 2 2 2.0 C=CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580909 120792 1 None -3 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 244 5 2 2 2.0 C=CCNC(=O)Cc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
127025787 137194 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 298 4 2 3 3.4 CCNC(=O)NCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
CHEMBL3759080 137194 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 298 4 2 3 3.4 CCNC(=O)NCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
44587357 187557 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 393 7 3 4 2.8 COc1ccc2[nH]c(CN3c4ccccc4CC3CO)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.07.012
CHEMBL498494 187557 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 393 7 3 4 2.8 COc1ccc2[nH]c(CN3c4ccccc4CC3CO)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.07.012
44358218 27294 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 289 4 2 3 1.9 CCCNC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL136895 27294 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 289 4 2 3 1.9 CCCNC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
86273222 120796 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 243 3 1 4 2.5 COc1ccc2[nH]cc(Cc3nc(C)no3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580913 120796 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 243 3 1 4 2.5 COc1ccc2[nH]cc(Cc3nc(C)no3)c2c1 10.1021/acs.jmedchem.5b00245
11515177 140516 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 314 5 1 3 3.4 COc1ccc2c(c1)c(C(C)(C)CNC(=O)C1CCC1)cn2C 10.1021/jm0512544
CHEMBL382439 140516 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 314 5 1 3 3.4 COc1ccc2c(c1)c(C(C)(C)CNC(=O)C1CCC1)cn2C 10.1021/jm0512544
122188348 122635 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 308 5 1 2 3.2 CC(=O)NCC1CCc2ccccc2N1CCc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612605 122635 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 308 5 1 2 3.2 CC(=O)NCC1CCc2ccccc2N1CCc1ccccc1 10.1021/acs.jmedchem.5b01066
10591657 4593 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 318 5 1 2 4.1 CCCC(=O)NCCc1c2n(c3ccccc13)Cc1ccccc1-2 10.1021/jm980684+
CHEMBL10328 4593 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 318 5 1 2 4.1 CCCC(=O)NCCc1c2n(c3ccccc13)Cc1ccccc1-2 10.1021/jm980684+
11616029 77625 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 272 4 1 3 2.4 COc1ccc2c(c1)c(C1(CNC(C)=O)CC1)cn2C 10.1021/jm0512544
CHEMBL209711 77625 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 272 4 1 3 2.4 COc1ccc2c(c1)c(C1(CNC(C)=O)CC1)cn2C 10.1021/jm0512544
16105170 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1021/jm800974d
CHEMBL515696 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1021/jm800974d
44264871 203311 0 None -26 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 297 5 1 3 4.2 CCCC(=O)Nc1ccc(Oc2cccc3c2CCO3)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7700 203311 0 None -26 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 297 5 1 3 4.2 CCCC(=O)Nc1ccc(Oc2cccc3c2CCO3)cc1 10.1016/j.bmcl.2003.11.030
10854190 97848 0 None -87 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 334 5 1 3 3.7 CCOc1ccc2c(c1)c(CCNC(C)=O)c1n2Cc2ccccc2-1 10.1021/jm980684+
CHEMBL274896 97848 0 None -87 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 334 5 1 3 3.7 CCOc1ccc2c(c1)c(CCNC(C)=O)c1n2Cc2ccccc2-1 10.1021/jm980684+
15453819 203265 0 None -30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 287 6 1 4 3.1 COCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7659 203265 0 None -30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 287 6 1 4 3.1 COCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
16105170 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1021/jm401343c
CHEMBL515696 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1021/jm401343c
16105170 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1021/jm800974d
CHEMBL515696 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1021/jm800974d
16105170 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1016/j.bmc.2008.07.012
CHEMBL515696 189125 0 None -4 2 Human 5.8 pKi = 5.8 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1016/j.bmc.2008.07.012
10447987 116455 1 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 308 5 1 3 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2-c1ccccc1 10.1021/jm020982d
CHEMBL33869 116455 1 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 308 5 1 3 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2-c1ccccc1 10.1021/jm020982d
90666303 108879 0 None -31 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 361 6 2 3 3.9 COc1ccc2[nH]c(Cn3ccc4ccccc43)c(CCNC(C)=O)c2c1 10.1039/C1MD00149C
CHEMBL3219324 108879 0 None -31 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 361 6 2 3 3.9 COc1ccc2[nH]c(Cn3ccc4ccccc43)c(CCNC(C)=O)c2c1 10.1039/C1MD00149C
23658145 156909 1 None -33 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
CHEMBL4079214 156909 1 None -33 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
10705590 206456 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 246 4 1 3 1.9 COc1ccc2cc(CCNC(C)=O)n(C)c2c1 10.1021/jm001125h
CHEMBL98484 206456 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 246 4 1 3 1.9 COc1ccc2cc(CCNC(C)=O)n(C)c2c1 10.1021/jm001125h
10705590 206456 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 246 4 1 3 1.9 COc1ccc2cc(CCNC(C)=O)n(C)c2c1 10.1021/jm970721h
CHEMBL98484 206456 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 246 4 1 3 1.9 COc1ccc2cc(CCNC(C)=O)n(C)c2c1 10.1021/jm970721h
16105170 189125 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1016/j.bmc.2009.04.068
CHEMBL515696 189125 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 405 5 1 5 3.3 COc1ccc2c(c1)CC1Cn3c(c(CCNC(C)=O)c4cc(OC)ccc43)CN21 10.1016/j.bmc.2009.04.068
22718521 16459 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 6 1 3 2.8 CCCc1nc2cccc(CCCNC(C)=O)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL124216 16459 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 6 1 3 2.8 CCCc1nc2cccc(CCCNC(C)=O)c2o1 10.1016/j.bmcl.2004.04.082
46885284 8006 0 None -114 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 251 7 1 3 2.2 CCOc1ccc(OC)cc1CCCNC(C)=O 10.1016/j.bmcl.2010.02.084
CHEMBL1091561 8006 0 None -114 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 251 7 1 3 2.2 CCOc1ccc(OC)cc1CCCNC(C)=O 10.1016/j.bmcl.2010.02.084
46884552 8028 0 None -1122 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 314 8 1 4 2.7 COc1ccc(OCc2ccccn2)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1091716 8028 0 None -1122 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 314 8 1 4 2.7 COc1ccc(OCc2ccccn2)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
122188233 122621 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2cc(OC)ccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612465 122621 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2cc(OC)ccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
145977894 163286 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 372 11 2 5 3.2 CC(=O)NCCN(C)c1cccc(OCCCCOc2cccc(O)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4206516 163286 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 372 11 2 5 3.2 CC(=O)NCCN(C)c1cccc(OCCCCOc2cccc(O)c2)c1 10.1021/acs.jmedchem.8b00893
10454621 101397 4 None -47 2 Human 5.7 pKi = 5.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 417 5 1 5 2.4 COc1ccc2c(c(CCNC(C)=O)c(I)n2C)c1[N+](=O)[O-] 10.1021/jm011053+
CHEMBL300728 101397 4 None -47 2 Human 5.7 pKi = 5.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 417 5 1 5 2.4 COc1ccc2c(c(CCNC(C)=O)c(I)n2C)c1[N+](=O)[O-] 10.1021/jm011053+
137636173 155448 0 None -63 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 276 6 1 3 2.3 COc1ccc2cccc(CCC(=O)NCCF)c2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4061905 155448 0 None -63 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 276 6 1 3 2.3 COc1ccc2cccc(CCC(=O)NCCF)c2n1 10.1016/j.ejmech.2016.12.013
71540275 85968 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 225 2 1 1 2.8 CC(=O)N[C@@H]1C[C@H]1c1cccc2ccccc12 10.1016/j.bmcl.2012.11.069
CHEMBL2314250 85968 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 225 2 1 1 2.8 CC(=O)N[C@@H]1C[C@H]1c1cccc2ccccc12 10.1016/j.bmcl.2012.11.069
18522208 126751 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 349 9 1 2 5.1 CC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL365852 126751 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 349 9 1 2 5.1 CC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
24750077 148500 0 None -691 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 314 7 1 4 3.0 COc1cccc(N(CCNC(C)=O)c2cccc(OC)c2)c1 10.1021/jm700957j
CHEMBL394273 148500 0 None -691 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 314 7 1 4 3.0 COc1cccc(N(CCNC(C)=O)c2cccc(OC)c2)c1 10.1021/jm700957j
10069719 192785 4 None 1 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 403 5 2 4 2.4 COc1ccc2[nH]c(I)c(CCNC(C)=O)c2c1[N+](=O)[O-] 10.1021/jm011053+
CHEMBL52559 192785 4 None 1 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 403 5 2 4 2.4 COc1ccc2[nH]c(I)c(CCNC(C)=O)c2c1[N+](=O)[O-] 10.1021/jm011053+
44429446 146187 0 None -14 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 288 6 1 3 3.0 CCCC(=O)NCCc1cn(C)c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL392422 146187 0 None -14 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 288 6 1 3 3.0 CCCC(=O)NCCc1cn(C)c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
56671856 64105 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 526 19 2 6 4.6 CC(=O)NCCN(C)c1cccc(OCCCCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813322 64105 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 526 19 2 6 4.6 CC(=O)NCCN(C)c1cccc(OCCCCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
16743294 91635 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 256 4 1 2 2.7 CC(=O)NCCCc1cn2c3c(cccc13)CCC2 10.1016/j.ejmech.2007.01.005
CHEMBL241928 91635 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 256 4 1 2 2.7 CC(=O)NCCCc1cn2c3c(cccc13)CCC2 10.1016/j.ejmech.2007.01.005
1550607 102581 64 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 298 6 0 3 4.9 CC(C)=CCC/C(C)=C/COc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
CHEMBL307341 102581 64 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 298 6 0 3 4.9 CC(C)=CCC/C(C)=C/COc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
44349269 16396 1 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 289 6 2 3 3.2 CCNC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL123972 16396 1 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 289 6 2 3 3.2 CCNC(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
10517621 206314 0 None -11 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 290 3 1 2 3.3 CC(=O)NCCc1c2n(c3ccccc13)Cc1ccccc1-2 10.1021/jm980684+
CHEMBL9765 206314 0 None -11 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 290 3 1 2 3.3 CC(=O)NCCc1c2n(c3ccccc13)Cc1ccccc1-2 10.1021/jm980684+
127039212 137487 0 None -154 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 360 5 1 4 4.3 COc1ccc2oc(-c3cccc4ccccc34)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3764879 137487 0 None -154 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 360 5 1 4 4.3 COc1ccc2oc(-c3cccc4ccccc34)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
10245336 38968 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 318 5 2 1 4.3 O=C(NCCc1c(-c2ccccc2)[nH]c2ccccc12)C1CCC1 10.1021/jm970721h
CHEMBL14701 38968 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 318 5 2 1 4.3 O=C(NCCc1c(-c2ccccc2)[nH]c2ccccc12)C1CCC1 10.1021/jm970721h
44389845 64486 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 377 10 1 2 4.9 O=C(NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2)C1CC1 10.1016/j.bmcl.2005.01.015
CHEMBL181974 64486 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 377 10 1 2 4.9 O=C(NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2)C1CC1 10.1016/j.bmcl.2005.01.015
20590652 129443 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 391 10 1 2 5.4 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL367604 129443 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 391 10 1 2 5.4 CCCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
44389813 130839 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 379 11 1 2 5.3 CCCC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL368886 130839 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 379 11 1 2 5.3 CCCC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
145991966 166272 0 None -5 3 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 285 3 1 3 3.2 COC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4285145 166272 0 None -5 3 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 285 3 1 3 3.2 COC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145987794 166556 0 None -19 3 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 298 4 2 2 3.2 CCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4290302 166556 0 None -19 3 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 298 4 2 2 3.2 CCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145988269 166626 0 None -10 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 326 5 2 2 3.8 CCCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4291381 166626 0 None -10 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 326 5 2 2 3.8 CCCNC(=O)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137639112 156298 0 None -10 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 245 4 2 3 1.5 COc1ccc2cccc(CCNC(N)=O)c2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4071572 156298 0 None -10 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 245 4 2 3 1.5 COc1ccc2cccc(CCNC(N)=O)c2n1 10.1016/j.ejmech.2016.12.013
137655238 158327 0 None -19 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 275 4 2 3 1.9 CNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4095210 158327 0 None -19 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 275 4 2 3 1.9 CNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
9805364 36717 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 484 11 2 4 4.8 CC(=O)NCCc1cccc2ccc(OCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
CHEMBL14514 36717 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 484 11 2 4 4.8 CC(=O)NCCc1cccc2ccc(OCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
9796251 117594 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCC(=O)NCCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
CHEMBL340745 117594 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCC(=O)NCCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
139451790 184704 13 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859295 184704 13 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
127026062 137151 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3oc(CNC(C)=O)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3758717 137151 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3oc(CNC(C)=O)cc3c2c1 10.1016/j.ejmech.2015.12.047
44394438 66615 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 375 9 1 2 5.6 CCC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL186736 66615 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 375 9 1 2 5.6 CCC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
44358238 118854 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 261 2 2 3 1.1 CNC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL344449 118854 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 261 2 2 3 1.1 CNC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
10333442 202179 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 272 6 1 3 2.7 CCCC(=O)NCCc1ccnc2ccc(OC)cc12 10.1016/S0960-894X(97)00392-2
CHEMBL68864 202179 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 272 6 1 3 2.7 CCCC(=O)NCCc1ccnc2ccc(OC)cc12 10.1016/S0960-894X(97)00392-2
139451776 184418 0 None 5 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 277 6 1 5 1.6 COc1ccc2nc(OC)n(CCCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
CHEMBL4854836 184418 0 None 5 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 277 6 1 5 1.6 COc1ccc2nc(OC)n(CCCNC(C)=O)c2c1 10.1021/acs.jmedchem.0c00627
10754723 168621 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 273 5 2 3 2.6 CCC(=O)NCCc1c(O)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
CHEMBL440692 168621 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 273 5 2 3 2.6 CCC(=O)NCCc1c(O)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
127040021 137479 0 None -24 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 360 5 1 4 4.3 COc1ccc2oc(-c3ccc4ccccc4c3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3764765 137479 0 None -24 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 360 5 1 4 4.3 COc1ccc2oc(-c3ccc4ccccc4c3)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
11776674 116136 1 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 246 4 1 3 1.9 COc1ccc2c(c1)c(CCNC(C)=O)cn2C 10.1021/jm020982d
CHEMBL33700 116136 1 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 246 4 1 3 1.9 COc1ccc2c(c1)c(CCNC(C)=O)cn2C 10.1021/jm020982d
10038243 116448 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 6 1 3 3.0 CCCC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL338659 116448 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 6 1 3 3.0 CCCC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
168274836 189544 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5173623 189544 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
10301190 8465 0 None 7 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 511 12 1 5 6.2 COC(=O)c1ccc(-c2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc2)cc1 10.1016/j.bmc.2010.04.008
CHEMBL1094545 8465 0 None 7 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 511 12 1 5 6.2 COC(=O)c1ccc(-c2ccc(OCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc2)cc1 10.1016/j.bmc.2010.04.008
137641357 156525 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.1 CC(=O)NCC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4074273 156525 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.1 CC(=O)NCC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
44394535 66663 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 390 8 1 3 5.1 CCC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
CHEMBL186977 66663 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 390 8 1 3 5.1 CCC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
86273228 120793 0 None -5 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 258 6 2 2 2.4 C=CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580910 120793 0 None -5 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 258 6 2 2 2.4 C=CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
11776674 116136 1 None -1 2 Human 8.6 pKi = 8.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 246 4 1 3 1.9 COc1ccc2c(c1)c(CCNC(C)=O)cn2C 10.1021/jm011053+
CHEMBL33700 116136 1 None -1 2 Human 8.6 pKi = 8.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 246 4 1 3 1.9 COc1ccc2c(c1)c(CCNC(C)=O)cn2C 10.1021/jm011053+
44394435 66578 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 361 8 1 2 5.2 CC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL186586 66578 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 361 8 1 2 5.2 CC(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
10561982 22805 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 239 3 1 1 3.0 CCC(=O)NCC1Cc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL133001 22805 0 None -12 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 239 3 1 1 3.0 CCC(=O)NCC1Cc2cccc3cccc1c23 10.1021/jm000922c
16094584 82818 0 None -33 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 281 5 1 2 3.3 COc1cccc(/C(=C/CNC(C)=O)c2ccccc2)c1 10.1021/jm060850a
CHEMBL218708 82818 0 None -33 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 281 5 1 2 3.3 COc1cccc(/C(=C/CNC(C)=O)c2ccccc2)c1 10.1021/jm060850a
44429441 86285 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 246 4 2 2 2.2 COc1cc(C)c2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.04.013
CHEMBL231872 86285 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 246 4 2 2 2.2 COc1cc(C)c2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.04.013
53237951 61675 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 333 5 1 2 3.7 CC(=O)NCCC1=C(Cc2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
CHEMBL1774518 61675 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 333 5 1 2 3.7 CC(=O)NCCC1=C(Cc2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
10332159 16600 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 246 5 1 3 2.6 CCC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL124577 16600 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 246 5 1 3 2.6 CCC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
127026423 137281 0 None -31 3 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 283 4 1 3 3.3 COc1ccc2ccc3occ(CCNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759802 137281 0 None -31 3 Human 8.6 pKi = 8.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 283 4 1 3 3.3 COc1ccc2ccc3occ(CCNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
44429443 144800 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 6 2 2 2.9 CCCC(=O)NCCc1c[nH]c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL391350 144800 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 6 2 2 2.9 CCCC(=O)NCCc1c[nH]c2c(C)cc(OC)cc12 10.1016/j.bmc.2007.04.013
9839199 21148 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
CHEMBL131424 21148 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 297 5 1 2 3.8 CCCC(=O)NCC1CCc2c(OC)ccc3cccc1c23 10.1021/jm000922c
137636079 155674 0 None -19 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 232 3 1 2 1.8 CCN1CC(CNC(C)=O)Cc2ccccc21 10.1021/acs.jmedchem.8b00359
CHEMBL4064626 155674 0 None -19 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 232 3 1 2 1.8 CCN1CC(CNC(C)=O)Cc2ccccc21 10.1021/acs.jmedchem.8b00359
127026425 137282 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3occ(CNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759816 137282 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 295 4 1 3 3.6 COc1ccc2ccc3occ(CNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
53310838 63445 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 321 4 1 4 2.8 CC(=O)NCCn1c(-c2ccccc2)nc2ccc3c(c21)CCO3 10.1021/jm200385u
CHEMBL1802021 63445 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 321 4 1 4 2.8 CC(=O)NCCn1c(-c2ccccc2)nc2ccc3c(c21)CCO3 10.1021/jm200385u
44424018 84920 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 620 16 4 8 4.2 COc1ccc2[nH]c(C(=O)OCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL226162 84920 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 620 16 4 8 4.2 COc1ccc2[nH]c(C(=O)OCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
56661499 64078 0 None 102 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 456 14 2 6 2.7 CC(=O)NCCN(C)c1cccc(OCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813174 64078 0 None 102 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 456 14 2 6 2.7 CC(=O)NCCN(C)c1cccc(OCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
46884555 8243 0 None -16 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 327 9 1 3 3.7 CCC(=O)NCCCc1ccc(OCc2ccccc2)c(OC)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1092911 8243 0 None -16 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 327 9 1 3 3.7 CCC(=O)NCCCc1ccc(OCc2ccccc2)c(OC)c1 10.1016/j.bmcl.2010.02.084
44358088 26561 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 246 2 1 3 1.3 CC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL136273 26561 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 246 2 1 3 1.3 CC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
10518621 96853 0 None -11 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 304 4 1 2 3.7 CCC(=O)NCCc1c2n(c3ccccc13)Cc1ccccc1-2 10.1021/jm980684+
CHEMBL269175 96853 0 None -11 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 304 4 1 2 3.7 CCC(=O)NCCc1c2n(c3ccccc13)Cc1ccccc1-2 10.1021/jm980684+
12985493 186499 0 None -213 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 363 7 1 3 4.3 COCc1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
CHEMBL491403 186499 0 None -213 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 363 7 1 3 4.3 COCc1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
10736247 206612 0 None -5 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 344 4 1 2 4.3 O=C(NCCc1c2n(c3ccccc13)CCc1ccccc1-2)C1CCC1 10.1021/jm980684+
CHEMBL9950 206612 0 None -5 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 344 4 1 2 4.3 O=C(NCCc1c2n(c3ccccc13)CCc1ccccc1-2)C1CCC1 10.1021/jm980684+
11208578 125355 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 292 2 1 2 3.0 CC(=O)NCC(=O)N1c2ccccc2C=Cc2ccccc21 10.1021/jm040768k
CHEMBL364845 125355 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 292 2 1 2 3.0 CC(=O)NCC(=O)N1c2ccccc2C=Cc2ccccc21 10.1021/jm040768k
189748 16622 6 None -60 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 262 5 2 3 1.9 COc1cc2[nH]cc(CCNC(C)=O)c2cc1OC 10.1021/jm401343c
CHEMBL124699 16622 6 None -60 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 262 5 2 3 1.9 COc1cc2[nH]cc(CCNC(C)=O)c2cc1OC 10.1021/jm401343c
11287002 15738 2 None -4 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)N[C@@H](C)COc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223275 15738 2 None -4 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)N[C@@H](C)COc1ccccc1 10.1016/j.bmc.2010.06.100
44358217 27290 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 287 3 2 3 1.7 O=C(NC1CC1)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL136894 27290 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 287 3 2 3 1.7 O=C(NC1CC1)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
44394456 65770 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 378 10 2 2 5.3 CCNC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL183962 65770 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 378 10 2 2 5.3 CCNC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
145963877 163693 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 503 14 2 5 5.7 CC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4211530 163693 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 503 14 2 5 5.7 CC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
10385056 111731 0 None -194 2 Human 7.7 pKi = 7.7 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 379 9 1 4 4.3 C=CCC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL329086 111731 0 None -194 2 Human 7.7 pKi = 7.7 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 379 9 1 4 4.3 C=CCC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm0005252
10385056 111731 0 None -194 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 379 9 1 4 4.3 C=CCC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm401343c
CHEMBL329086 111731 0 None -194 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 379 9 1 4 4.3 C=CCC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm401343c
145 140 48 None -40 30 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1832 140 48 None -40 30 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
CHEMBL7257 140 48 None -40 30 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
DB14010 140 48 None -40 30 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
122178507 120797 0 None -13 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 243 3 1 4 2.5 COc1ccc2[nH]cc(Cc3nnc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580915 120797 0 None -13 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 243 3 1 4 2.5 COc1ccc2[nH]cc(Cc3nnc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
127025170 137204 0 None -4 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 312 5 2 3 3.5 CCNC(=O)NCCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
CHEMBL3759180 137204 0 None -4 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 312 5 2 3 3.5 CCNC(=O)NCCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
162656758 180330 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 259 5 1 4 1.7 CCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
CHEMBL4757920 180330 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 259 5 1 4 1.7 CCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
162658247 180426 0 None -2 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 245 4 1 4 1.3 COc1ccc2cnnc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4759137 180426 0 None -2 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 245 4 1 4 1.3 COc1ccc2cnnc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
11688043 77626 0 None -28 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 6 1 3 3.1 CCCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CC1 10.1021/jm0512544
CHEMBL209712 77626 0 None -28 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 6 1 3 3.1 CCCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CC1 10.1021/jm0512544
122188234 122622 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2ccc(OC)cc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612466 122622 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 338 6 1 3 3.5 CCC(=O)NCC1CCc2ccc(OC)cc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
44424019 84921 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 648 18 4 8 5.0 COc1ccc2[nH]c(C(=O)OCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL226163 84921 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 648 18 4 8 5.0 COc1ccc2[nH]c(C(=O)OCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
16094595 82834 4 None -407 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 283 6 1 2 3.4 COc1cccc(C(CCNC(C)=O)c2ccccc2)c1 10.1021/jm060850a
CHEMBL218773 82834 4 None -407 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 283 6 1 2 3.4 COc1cccc(C(CCNC(C)=O)c2ccccc2)c1 10.1021/jm060850a
44412078 138974 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 272 3 2 3 2.4 CC(=O)NCC1(c2cn(C)c3ccc(O)cc23)CCC1 10.1021/jm0512544
CHEMBL379504 138974 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 272 3 2 3 2.4 CC(=O)NCC1(c2cn(C)c3ccc(O)cc23)CCC1 10.1021/jm0512544
137637884 155693 0 None -10 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.3 CCC(=O)NC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4064813 155693 0 None -10 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.3 CCC(=O)NC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
122188352 122638 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 263 3 2 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612609 122638 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 263 3 2 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
44394532 66895 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 376 7 1 3 4.7 CC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
CHEMBL188016 66895 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 376 7 1 3 4.7 CC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
11351216 62060 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 441 6 1 3 5.4 O=C(CBr)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779807 62060 0 None -4 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 441 6 1 3 5.4 O=C(CBr)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
162668689 182166 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 285 5 1 4 2.2 COc1ccc2nc(C3CC3)nc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4790145 182166 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 285 5 1 4 2.2 COc1ccc2nc(C3CC3)nc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
71508233 86632 0 None -40 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 355 10 1 3 3.9 CCC(=O)NCCCc1cc(OC)ccc1CCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326201 86632 0 None -40 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 355 10 1 3 3.9 CCC(=O)NCCCc1cc(OC)ccc1CCc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
11066802 99612 0 None -21 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 308 5 1 3 3.7 CCC(=O)NCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm001125h
CHEMBL287343 99612 0 None -21 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 308 5 1 3 3.7 CCC(=O)NCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm001125h
11463056 62058 0 None -51 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 1 3 5.4 CCC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779805 62058 0 None -51 2 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 1 3 5.4 CCC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
11131123 170056 0 None -12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 323 6 1 3 3.7 COc1cccc(Cc2oc3ccccc3c2CCNC(C)=O)c1 10.1021/jm0005252
CHEMBL445117 170056 0 None -12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 323 6 1 3 3.7 COc1cccc(Cc2oc3ccccc3c2CCNC(C)=O)c1 10.1021/jm0005252
16094593 165480 0 None -91 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 281 5 1 2 3.3 COc1cccc(/C(=C\CNC(C)=O)c2ccccc2)c1 10.1021/jm060850a
CHEMBL425644 165480 0 None -91 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 281 5 1 2 3.3 COc1cccc(/C(=C\CNC(C)=O)c2ccccc2)c1 10.1021/jm060850a
44349305 170560 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 320 6 1 3 4.0 O=C(NCCCc1cccc2nc(-c3ccccc3)oc12)C1CC1 10.1016/j.bmcl.2004.04.082
CHEMBL445840 170560 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 320 6 1 3 4.0 O=C(NCCCc1cccc2nc(-c3ccccc3)oc12)C1CC1 10.1016/j.bmcl.2004.04.082
23725513 125314 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@H]1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL3648357 125314 0 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 258 3 1 3 2.7 CC(=O)NCC[C@H]1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
44394416 65891 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 389 9 1 2 5.9 CC(C)C(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL184562 65891 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 389 9 1 2 5.9 CC(C)C(=O)NC[C@@H]1CC1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
10750842 188087 3 None -30 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 207 5 1 2 1.8 COc1cccc(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
CHEMBL50398 188087 3 None -30 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 207 5 1 2 1.8 COc1cccc(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
127026426 137262 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 309 5 1 3 3.7 COc1ccc2ccc3occ(CCNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759606 137262 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 309 5 1 3 3.7 COc1ccc2ccc3occ(CCNC(=O)C4CC4)c3c2c1 10.1016/j.ejmech.2015.12.047
90666307 108883 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 389 8 2 3 3.9 C=CCC(=O)NCCc1c(CN2Cc3ccccc3C2)[nH]c2ccc(OC)cc12 10.1039/C1MD00149C
CHEMBL3219328 108883 0 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 389 8 2 3 3.9 C=CCC(=O)NCCc1c(CN2Cc3ccccc3C2)[nH]c2ccc(OC)cc12 10.1039/C1MD00149C
16094584 82818 0 None -33 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 281 5 1 2 3.3 COc1cccc(/C(=C/CNC(C)=O)c2ccccc2)c1 10.1021/jm800974d
CHEMBL218708 82818 0 None -33 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 281 5 1 2 3.3 COc1cccc(/C(=C/CNC(C)=O)c2ccccc2)c1 10.1021/jm800974d
86079062 180140 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 245 4 1 4 1.3 COc1ccc2ncnc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4755860 180140 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 245 4 1 4 1.3 COc1ccc2ncnc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
10808489 206030 0 None -42 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 360 6 1 3 4.1 CCOc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2Cc2ccccc2-1 10.1021/jm980684+
CHEMBL9600 206030 0 None -42 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 360 6 1 3 4.1 CCOc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2Cc2ccccc2-1 10.1021/jm980684+
53231464 62062 0 None -21 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 375 6 1 3 5.2 C=CC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779809 62062 0 None -21 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 375 6 1 3 5.2 C=CC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
11173131 123566 0 None -7 2 Human 6.6 pKi = 6.6 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 265 2 1 1 3.1 CC(=O)NCC1Cc2ccccc2Cc2ccccc21 10.1021/jm040768k
CHEMBL363321 123566 0 None -7 2 Human 6.6 pKi = 6.6 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 265 2 1 1 3.1 CC(=O)NCC1Cc2ccccc2Cc2ccccc21 10.1021/jm040768k
11014883 206377 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 400 6 1 3 4.1 COc1ccc2c(Br)c(CCNC(C)=O)n(Cc3ccccc3)c2c1 10.1021/jm001125h
CHEMBL98028 206377 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 400 6 1 3 4.1 COc1ccc2c(Br)c(CCNC(C)=O)n(Cc3ccccc3)c2c1 10.1021/jm001125h
22718576 114094 0 None -4 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 1 3 2.2 CC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL333810 114094 0 None -4 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 4 1 3 2.2 CC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
11824365 106870 0 None -47 2 Human 7.6 pKi = 7.6 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1ccc(Cc2oc3ccc(OC)cc3c2CCNC(C)=O)cc1 10.1021/jm0005252
CHEMBL317742 106870 0 None -47 2 Human 7.6 pKi = 7.6 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1ccc(Cc2oc3ccc(OC)cc3c2CCNC(C)=O)cc1 10.1021/jm0005252
44424021 141547 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 690 21 4 8 6.2 COc1ccc2[nH]c(C(=O)OCCCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL388141 141547 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 690 21 4 8 6.2 COc1ccc2[nH]c(C(=O)OCCCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
53231465 62056 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 237 3 1 2 2.7 CC(=O)NCCc1csc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779803 62056 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 237 3 1 2 2.7 CC(=O)NCCc1csc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
44579260 186522 0 None -38 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 377 6 1 4 4.0 COC(=O)c1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
CHEMBL491605 186522 0 None -38 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 377 6 1 4 4.0 COC(=O)c1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
10853021 97672 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 318 3 1 2 3.9 CC(=O)NCCc1c2n(c3ccccc13)CCCc1ccccc1-2 10.1021/jm980684+
CHEMBL273623 97672 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 318 3 1 2 3.9 CC(=O)NCCc1c2n(c3ccccc13)CCCc1ccccc1-2 10.1021/jm980684+
10465460 206555 2 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 202 3 2 1 1.8 CC(=O)NCCc1cc2ccccc2[nH]1 10.1021/jm001125h
CHEMBL99083 206555 2 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 202 3 2 1 1.8 CC(=O)NCCc1cc2ccccc2[nH]1 10.1021/jm001125h
10465460 206555 2 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 202 3 2 1 1.8 CC(=O)NCCc1cc2ccccc2[nH]1 10.1021/jm970721h
CHEMBL99083 206555 2 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 202 3 2 1 1.8 CC(=O)NCCc1cc2ccccc2[nH]1 10.1021/jm970721h
137656715 158988 0 None -5 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 308 5 1 2 3.0 CC(=O)NCC1Cc2ccccc2N(CCc2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4102517 158988 0 None -5 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 308 5 1 2 3.0 CC(=O)NCC1Cc2ccccc2N(CCc2ccccc2)C1 10.1021/acs.jmedchem.8b00359
71540393 85972 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 226 2 2 1 2.7 CNC(=O)N/C=C/c1cccc2ccccc12 10.1016/j.bmcl.2012.11.069
CHEMBL2314254 85972 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 226 2 2 1 2.7 CNC(=O)N/C=C/c1cccc2ccccc12 10.1016/j.bmcl.2012.11.069
127038130 136087 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 347 8 1 2 4.5 CC(=O)NCCc1cccc2ccc(OCCCc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3739824 136087 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 347 8 1 2 4.5 CC(=O)NCCc1cccc2ccc(OCCCc3ccccc3)cc12 10.1039/C5MD00190K
44424022 83045 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 718 23 4 8 6.9 COc1ccc2[nH]c(C(=O)OCCCCCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL220091 83045 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 718 23 4 8 6.9 COc1ccc2[nH]c(C(=O)OCCCCCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
10737123 96918 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 358 4 1 2 4.7 O=C(NCCc1c2n(c3ccccc13)CCCc1ccccc1-2)C1CCC1 10.1021/jm980684+
CHEMBL269670 96918 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 358 4 1 2 4.7 O=C(NCCc1c2n(c3ccccc13)CCCc1ccccc1-2)C1CCC1 10.1021/jm980684+
90666302 108878 0 None -11 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.4 COc1ccc2[nH]c(CN3CCc4ccccc4C3)c(CCNC(C)=O)c2c1 10.1039/C1MD00149C
CHEMBL3219323 108878 0 None -11 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.4 COc1ccc2[nH]c(CN3CCc4ccccc4C3)c(CCNC(C)=O)c2c1 10.1039/C1MD00149C
CHEMBL3109562 209334 0 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 minsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 mins
ChEMBL None None None CCC1=C(C)C2=Cc3c(CCNC(C)=O)c4cc(OC)ccc4n3[B-](F)(F)[N+]2=C1C 10.1021/ml4004155
10596576 4094 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 390 7 1 3 5.1 CCCC(=O)NCCc1c2n(c3ccc(OCC)cc13)CCCc1ccccc1-2 10.1021/jm980684+
CHEMBL10007 4094 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 390 7 1 3 5.1 CCCC(=O)NCCc1c2n(c3ccc(OCC)cc13)CCCc1ccccc1-2 10.1021/jm980684+
46884598 8091 0 None -20 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 223 5 2 3 1.5 COc1cc(CCCNC(C)=O)ccc1O 10.1016/j.bmcl.2010.02.084
CHEMBL1092047 8091 0 None -20 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 223 5 2 3 1.5 COc1cc(CCCNC(C)=O)ccc1O 10.1016/j.bmcl.2010.02.084
45269177 193186 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 299 5 1 3 2.5 CCCC(=O)NCCc1c2n(c3ccccc13)CCN(C)C2 10.1016/j.bmc.2009.04.068
CHEMBL540182 193186 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 299 5 1 3 2.5 CCCC(=O)NCCc1c2n(c3ccccc13)CCN(C)C2 10.1016/j.bmc.2009.04.068
45269183 194341 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 385 7 2 3 4.1 COc1ccc2[nH]c(CN(C)c3ccc(Cl)cc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
CHEMBL560186 194341 0 None -6 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 385 7 2 3 4.1 COc1ccc2[nH]c(CN(C)c3ccc(Cl)cc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2009.04.068
16094594 82819 0 None -165 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 321 6 1 2 4.0 COc1cccc(/C(=C\CNC(=O)C2CCC2)c2ccccc2)c1 10.1021/jm060850a
CHEMBL218709 82819 0 None -165 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 321 6 1 2 4.0 COc1cccc(/C(=C\CNC(=O)C2CCC2)c2ccccc2)c1 10.1021/jm060850a
162674581 182720 0 None -51 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 268 3 1 4 2.7 COc1ccc2cccc(/C=C/c3n[nH]c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
CHEMBL4797226 182720 0 None -51 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 268 3 1 4 2.7 COc1ccc2cccc(/C=C/c3n[nH]c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
46885227 7975 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 327 9 1 3 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1ccccc1 10.1016/j.bmcl.2010.02.084
CHEMBL1091161 7975 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 327 9 1 3 3.7 CCC(=O)NCCCc1cc(OC)ccc1OCc1ccccc1 10.1016/j.bmcl.2010.02.084
16743464 91880 0 None -11 2 Human 5.6 pKi = 5.6 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 310 3 1 2 3.9 CC(=O)NCC1(c2cn3c4c(cccc24)CCC3)CCCCC1 10.1016/j.ejmech.2007.01.005
CHEMBL243002 91880 0 None -11 2 Human 5.6 pKi = 5.6 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 310 3 1 2 3.9 CC(=O)NCC1(c2cn3c4c(cccc24)CCC3)CCCCC1 10.1016/j.ejmech.2007.01.005
10714573 98028 0 None -12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCOc1ccc2c(c1)c(CCNC(=O)CC)c1n2CCCc2ccccc2-1 10.1021/jm980684+
CHEMBL276005 98028 0 None -12 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCOc1ccc2c(c1)c(CCNC(=O)CC)c1n2CCCc2ccccc2-1 10.1021/jm980684+
1353 3368 3 None -112 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm800974d
9998187 3368 3 None -112 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm800974d
CHEMBL33549 3368 3 None -112 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm800974d
145976375 163234 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 525 15 2 6 5.7 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2cccc(OC(=O)NC3CCCCC3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4206000 163234 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 525 15 2 6 5.7 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2cccc(OC(=O)NC3CCCCC3)c2)c1 10.1021/acs.jmedchem.8b00893
46885288 8230 0 None -95 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 343 9 1 4 3.4 COc1ccc(COc2ccc(OC)cc2CCCNC(C)=O)cc1 10.1016/j.bmcl.2010.02.084
CHEMBL1092839 8230 0 None -95 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 343 9 1 4 3.4 COc1ccc(COc2ccc(OC)cc2CCCNC(C)=O)cc1 10.1016/j.bmcl.2010.02.084
10760155 97954 0 None -43 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 4 1 3 3.9 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCCc2ccccc2-1 10.1021/jm980684+
CHEMBL275529 97954 0 None -43 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 4 1 3 3.9 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCCc2ccccc2-1 10.1021/jm980684+
7922 1917 0 None -741 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 349 6 2 3 3.7 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)CO 10.1016/j.bmc.2008.08.052
9798456 1917 0 None -741 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 349 6 2 3 3.7 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)CO 10.1016/j.bmc.2008.08.052
CHEMBL476131 1917 0 None -741 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 349 6 2 3 3.7 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)CO 10.1016/j.bmc.2008.08.052
11045144 206531 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 310 4 2 2 3.0 CCC(=O)NCc1[nH]c2cc(OC)ccc2c1Br 10.1021/jm001125h
CHEMBL98956 206531 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 310 4 2 2 3.0 CCC(=O)NCc1[nH]c2cc(OC)ccc2c1Br 10.1021/jm001125h
49865205 15661 0 None -4 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(S[C@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223052 15661 0 None -4 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(S[C@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
137644121 157592 0 None -7 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 291 4 1 1 4.0 CCC(=O)NCC1=C(c2ccccc2)c2ccccc2CC1 10.1021/acs.jmedchem.8b00359
CHEMBL4087265 157592 0 None -7 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 291 4 1 1 4.0 CCC(=O)NCC1=C(c2ccccc2)c2ccccc2CC1 10.1021/acs.jmedchem.8b00359
11702296 64645 4 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 1 4 2.7 COc1ccc2nc(-c3ccccc3)c(CCNC(C)=O)n2c1 10.1016/j.ejmech.2011.06.030
CHEMBL1823017 64645 4 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 1 4 2.7 COc1ccc2nc(-c3ccccc3)c(CCNC(C)=O)n2c1 10.1016/j.ejmech.2011.06.030
86273223 120794 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 242 3 1 3 3.1 COc1ccc2[nH]cc(Cc3ncc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580911 120794 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 242 3 1 3 3.1 COc1ccc2[nH]cc(Cc3ncc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
90666305 108881 0 None -125 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2[nH]c(CN3Cc4ccccc4C3)c(CCNC(C)=O)c2c1 10.1039/C1MD00149C
CHEMBL3219326 108881 0 None -125 2 Human 6.6 pKi = 6.6 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2[nH]c(CN3Cc4ccccc4C3)c(CCNC(C)=O)c2c1 10.1039/C1MD00149C
49865266 15684 2 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 225 5 1 3 1.9 COc1ccc(SCCNC(C)=O)cc1 10.1016/j.bmc.2010.06.100
CHEMBL1223126 15684 2 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 225 5 1 3 1.9 COc1ccc(SCCNC(C)=O)cc1 10.1016/j.bmc.2010.06.100
10520058 97673 0 None -8 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 324 3 1 2 4.0 CC(=O)NCCc1c2n(c3ccc(Cl)cc13)Cc1ccccc1-2 10.1021/jm980684+
CHEMBL273624 97673 0 None -8 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 324 3 1 2 4.0 CC(=O)NCCc1c2n(c3ccc(Cl)cc13)Cc1ccccc1-2 10.1021/jm980684+
53231367 62061 0 None -117 2 Human 5.5 pKi = 5.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 425 8 1 3 6.0 O=C(CCCCl)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779808 62061 0 None -117 2 Human 5.5 pKi = 5.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 425 8 1 3 6.0 O=C(CCCCl)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
11078652 206171 0 None -16 2 Human 6.5 pKi = 6.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 351 7 1 3 4.3 CCc1ccc2oc(Cc3cccc(OC)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL96778 206171 0 None -16 2 Human 6.5 pKi = 6.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 351 7 1 3 4.3 CCc1ccc2oc(Cc3cccc(OC)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
10641756 97813 0 None -57 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 352 3 1 2 4.6 CC(=O)NCCc1c2n(c3ccc(Cl)cc13)CCCc1ccccc1-2 10.1021/jm980684+
CHEMBL274630 97813 0 None -57 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 352 3 1 2 4.6 CC(=O)NCCc1c2n(c3ccc(Cl)cc13)CCCc1ccccc1-2 10.1021/jm980684+
56662799 64110 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 526 15 2 6 2.9 COc1cccc(N(CCNC(C)=O)C(=O)CCCCC(=O)N(CCNC(C)=O)c2cccc(OC)c2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813327 64110 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 526 15 2 6 2.9 COc1cccc(N(CCNC(C)=O)C(=O)CCCCC(=O)N(CCNC(C)=O)c2cccc(OC)c2)c1 10.1016/j.bmc.2011.06.063
11088627 205801 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 324 6 1 4 3.1 COc1ccc2oc(Cc3cccnc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL94745 205801 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 324 6 1 4 3.1 COc1ccc2oc(Cc3cccnc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
15453821 203385 0 None -151 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 301 6 1 3 4.6 CCCC(=O)Nc1ccc(Sc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7771 203385 0 None -151 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 301 6 1 3 4.6 CCCC(=O)Nc1ccc(Sc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
145983175 165867 0 None -14 3 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 314 4 2 2 3.4 CCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4277390 165867 0 None -14 3 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 314 4 2 2 3.4 CCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137661786 158557 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 262 5 1 3 1.9 COc1cnc2cccc(CCNC(=O)CF)c2c1 10.1016/j.ejmech.2016.12.013
CHEMBL4097693 158557 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 262 5 1 3 1.9 COc1cnc2cccc(CCNC(=O)CF)c2c1 10.1016/j.ejmech.2016.12.013
145975938 163336 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 519 14 3 6 5.4 CC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3cccc(O)c3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4207166 163336 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 519 14 3 6 5.4 CC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3cccc(O)c3)c2)c1 10.1021/acs.jmedchem.8b00893
122188239 122627 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 320 5 1 2 3.5 O=C(NCC1CCc2ccccc2N1Cc1ccccc1)C1CC1 10.1021/acs.jmedchem.5b01066
CHEMBL3612471 122627 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 320 5 1 2 3.5 O=C(NCC1CCc2ccccc2N1Cc1ccccc1)C1CC1 10.1021/acs.jmedchem.5b01066
46885286 8069 0 None -218 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 327 9 1 3 3.4 COc1ccc(OCCc2ccccc2)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1091895 8069 0 None -218 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 327 9 1 3 3.4 COc1ccc(OCCc2ccccc2)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
10620323 206589 0 None -34 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 388 6 1 3 4.7 CCOc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2CCCc2ccccc2-1 10.1021/jm980684+
CHEMBL9935 206589 0 None -34 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 388 6 1 3 4.7 CCOc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2CCCc2ccccc2-1 10.1021/jm980684+
10658090 206543 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 246 5 2 2 2.2 COc1ccc2[nH]c(CCCNC(C)=O)cc2c1 10.1021/jm001125h
CHEMBL99000 206543 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 246 5 2 2 2.2 COc1ccc2[nH]c(CCCNC(C)=O)cc2c1 10.1021/jm001125h
10658090 206543 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 246 5 2 2 2.2 COc1ccc2[nH]c(CCCNC(C)=O)cc2c1 10.1021/jm970721h
CHEMBL99000 206543 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 246 5 2 2 2.2 COc1ccc2[nH]c(CCCNC(C)=O)cc2c1 10.1021/jm970721h
12985490 180628 0 None -12 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 349 6 2 3 3.7 COc1ccc2cc(-c3ccc(CO)cc3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL476132 180628 0 None -12 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 349 6 2 3 3.7 COc1ccc2cc(-c3ccc(CO)cc3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
10015474 18358 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 5 1 3 2.8 Cc1nc2cccc(CCCNC(=O)C(C)C)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL127596 18358 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 5 1 3 2.8 Cc1nc2cccc(CCCNC(=O)C(C)C)c2o1 10.1016/j.bmcl.2004.04.082
145979282 166111 0 None -16 3 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4281915 166111 0 None -16 3 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
53238408 61682 0 None -81 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 349 5 1 3 3.6 COc1ccc(C2=C(CCNC(C)=O)c3c(ccc4c3CCO4)C2)cc1 10.1021/jm200221q
CHEMBL1774527 61682 0 None -81 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 349 5 1 3 3.6 COc1ccc(C2=C(CCNC(C)=O)c3c(ccc4c3CCO4)C2)cc1 10.1021/jm200221q
11426853 165804 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 309 3 1 3 2.7 COc1ccc2c(c1)C(CNC(C)=O)Cc1ccccc1C2=O 10.1021/jm040768k
CHEMBL427516 165804 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 309 3 1 3 2.7 COc1ccc2c(c1)C(CNC(C)=O)Cc1ccccc1C2=O 10.1021/jm040768k
137641357 156525 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.1 CC(=O)NCC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4074273 156525 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 280 3 1 2 3.1 CC(=O)NCC1Cc2ccccc2N(c2ccccc2)C1 10.1021/acs.jmedchem.8b00359
49865321 15707 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 251 7 1 3 2.4 CCCC(=O)NC[C@H](C)Oc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223195 15707 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 251 7 1 3 2.4 CCCC(=O)NC[C@H](C)Oc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
44272406 68825 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 289 5 3 3 2.7 CCNC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CC)N2 10.1016/j.bmcl.2003.12.052
CHEMBL19260 68825 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 289 5 3 3 2.7 CCNC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(CC)N2 10.1016/j.bmcl.2003.12.052
1355 3371 3 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9806449 3371 3 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL14453 3371 3 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
71540395 85975 0 None 2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 256 3 2 2 2.7 CNC(=O)N/C=C/c1c(OC)ccc2ccccc12 10.1016/j.bmcl.2012.11.069
CHEMBL2314258 85975 0 None 2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 256 3 2 2 2.7 CNC(=O)N/C=C/c1c(OC)ccc2ccccc12 10.1016/j.bmcl.2012.11.069
11810280 206183 0 None -16 2 Human 8.5 pKi = 8.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 351 8 1 3 4.5 CCCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL96859 206183 0 None -16 2 Human 8.5 pKi = 8.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 351 8 1 3 4.5 CCCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
10091075 17084 0 None 8 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 378 11 1 3 5.2 CCCC(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL125705 17084 0 None 8 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 378 11 1 3 5.2 CCCC(=O)NCCCc1cccc2nc(CCCCc3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
52918078 60415 0 None -11 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 247 5 1 4 1.6 CCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
CHEMBL1760946 60415 0 None -11 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 247 5 1 4 1.6 CCC(=O)NCCn1ccc2ccc(OC)nc21 10.1016/j.bmcl.2011.02.097
23658146 156564 1 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
CHEMBL4074895 156564 1 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 6 2 3 2.5 CCC(=O)NC[C@H](CO)c1cccc2ccc(OC)cc12 10.1039/C4MD00149D
56664925 64104 0 None 53 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 498 17 2 6 3.8 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813321 64104 0 None 53 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 498 17 2 6 3.8 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
137631636 156055 0 None -7 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 308 4 1 2 3.4 CCC(=O)NC[C@@H]1CN(C)c2ccccc2[C@@H]1c1ccccc1 10.1021/acs.jmedchem.8b00359
CHEMBL4068887 156055 0 None -7 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 308 4 1 2 3.4 CCC(=O)NC[C@@H]1CN(C)c2ccccc2[C@@H]1c1ccccc1 10.1021/acs.jmedchem.8b00359
85880795 110366 0 None 12 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 319 9 1 3 4.0 CCCCCCOc1ccc2c(c1)C(CCNC(C)=O)CCO2 10.1021/jm401343c
CHEMBL3260984 110366 0 None 12 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 319 9 1 3 4.0 CCCCCCOc1ccc2c(c1)C(CCNC(C)=O)CCO2 10.1021/jm401343c
18360658 8787 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 518 13 2 5 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4scc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1097497 8787 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 518 13 2 5 5.7 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4scc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
10015475 16569 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 6 1 3 2.8 CCC(=O)NCCCc1cccc2nc(CC)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL124362 16569 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 260 6 1 3 2.8 CCC(=O)NCCCc1cccc2nc(CC)oc12 10.1016/j.bmcl.2004.04.082
44272444 67589 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 303 6 3 3 3.0 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)NCC)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL19109 67589 0 None -3 2 Human 8.5 pKi = 8.5 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 303 6 3 3 3.0 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)NCC)c2O1 10.1016/j.bmcl.2003.12.052
137648419 157285 0 None -15 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 293 4 1 1 3.9 CCC(=O)NC[C@@H]1CCc2ccccc2[C@@H]1c1ccccc1 10.1021/acs.jmedchem.8b00359
CHEMBL4083618 157285 0 None -15 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 293 4 1 1 3.9 CCC(=O)NC[C@@H]1CCc2ccccc2[C@@H]1c1ccccc1 10.1021/acs.jmedchem.8b00359
10926138 206228 0 None -57 2 Human 8.5 pKi = 8.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 349 8 1 3 4.3 C=CCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL97186 206228 0 None -57 2 Human 8.5 pKi = 8.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 349 8 1 3 4.3 C=CCC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
44429447 87304 0 None -5 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 310 4 2 2 2.6 COc1cc(Br)c2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.04.013
CHEMBL233728 87304 0 None -5 2 Human 8.5 pKi = 8.5 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 310 4 2 2 2.6 COc1cc(Br)c2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.04.013
139451784 184803 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 317 7 1 5 2.4 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CCC1 10.1021/acs.jmedchem.0c00627
CHEMBL4860729 184803 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 317 7 1 5 2.4 CCOc1nc2ccc(OC)cc2n1CCNC(=O)C1CCC1 10.1021/acs.jmedchem.0c00627
49865149 15642 2 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OC(C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1222986 15642 2 None 2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OC(C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
25270146 30463 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 262 5 1 3 2.2 CCCC(=O)N[C@H]1CCN(c2cccc(OC)c2)C1 10.1016/j.bmcl.2003.09.030
CHEMBL139497 30463 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 262 5 1 3 2.2 CCCC(=O)N[C@H]1CCN(c2cccc(OC)c2)C1 10.1016/j.bmcl.2003.09.030
15453093 85970 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 255 3 1 2 2.8 COc1ccc2ccccc2c1[C@@H]1C[C@H]1NC(C)=O 10.1016/j.bmcl.2012.11.069
CHEMBL2314252 85970 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 255 3 1 2 2.8 COc1ccc2ccccc2c1[C@@H]1C[C@H]1NC(C)=O 10.1016/j.bmcl.2012.11.069
10022490 66707 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 377 10 1 2 5.7 CC(C)C(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL187186 66707 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 377 10 1 2 5.7 CC(C)C(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
49865324 15710 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 267 7 1 3 3.1 CCCC(=O)NC[C@H](C)Sc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223198 15710 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 267 7 1 3 3.1 CCCC(=O)NC[C@H](C)Sc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
9860296 28989 0 None 8 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 272 3 1 3 1.7 O=C(N[C@@H]1CCN(c2cccc3c2CCO3)C1)C1CC1 10.1016/j.bmcl.2003.09.030
CHEMBL138228 28989 0 None 8 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 272 3 1 3 1.7 O=C(N[C@@H]1CCN(c2cccc3c2CCO3)C1)C1CC1 10.1016/j.bmcl.2003.09.030
18466111 19630 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
CHEMBL130214 19630 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 5 1 2 3.4 CCCC(=O)NCC1Cc2cccc3ccc(OC)c1c23 10.1021/jm000922c
1362 3370 18 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9870523 3370 18 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL429392 3370 18 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
56653120 110367 0 None 12 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 336 8 2 2 3.9 CC(=O)NCCc1c[nH]c2ccc(OCCCc3ccccc3)cc12 10.1021/jm401343c
CHEMBL3260985 110367 0 None 12 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 336 8 2 2 3.9 CC(=O)NCCc1c[nH]c2ccc(OCCCc3ccccc3)cc12 10.1021/jm401343c
56681902 64106 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 554 21 2 6 5.4 CC(=O)NCCN(C)c1cccc(OCCCCCCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813323 64106 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 554 21 2 6 5.4 CC(=O)NCCN(C)c1cccc(OCCCCCCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
22718532 16589 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 218 4 1 3 1.9 CC(=O)NCCCc1cccc2ncoc12 10.1016/j.bmcl.2004.04.082
CHEMBL124488 16589 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 218 4 1 3 1.9 CC(=O)NCCCc1cccc2ncoc12 10.1016/j.bmcl.2004.04.082
9881917 96581 0 None -44 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 271 5 1 3 3.8 CCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL266970 96581 0 None -44 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 271 5 1 3 3.8 CCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
25210000 188894 0 None -11 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 408 7 2 5 3.3 COc1ccc2[nH]c(CN3CCc4ccc([N+](=O)[O-])cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL513933 188894 0 None -11 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 408 7 2 5 3.3 COc1ccc2[nH]c(CN3CCc4ccc([N+](=O)[O-])cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
25022442 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1021/jm800974d
CHEMBL514413 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1021/jm800974d
11681201 140532 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 314 5 1 3 3.5 CCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCCC1 10.1021/jm0512544
CHEMBL382555 140532 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 314 5 1 3 3.5 CCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCCC1 10.1021/jm0512544
162663385 181406 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 271 5 1 4 1.7 COc1ccc2cnnc(CCNC(=O)C3CC3)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4780509 181406 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 271 5 1 4 1.7 COc1ccc2cnnc(CCNC(=O)C3CC3)c2c1 10.1016/j.ejmech.2020.112078
122188229 122617 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 249 3 3 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612460 122617 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 249 3 3 2 1.9 CCNC(=S)NCC1CCc2ccccc2N1 10.1021/acs.jmedchem.5b01066
11573203 140534 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 312 5 1 3 3.1 COc1ccc2c(c1)c(C1(CNC(=O)C3CC3)CCC1)cn2C 10.1021/jm0512544
CHEMBL382579 140534 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 312 5 1 3 3.1 COc1ccc2c(c1)c(C1(CNC(=O)C3CC3)CCC1)cn2C 10.1021/jm0512544
10991315 206544 0 None -23 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 336 7 1 3 4.1 CCC(=O)NCCCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm001125h
CHEMBL99001 206544 0 None -23 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 336 7 1 3 4.1 CCC(=O)NCCCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm001125h
25210000 188894 0 None -11 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 408 7 2 5 3.3 COc1ccc2[nH]c(CN3CCc4ccc([N+](=O)[O-])cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL513933 188894 0 None -11 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 408 7 2 5 3.3 COc1ccc2[nH]c(CN3CCc4ccc([N+](=O)[O-])cc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
145974583 163927 0 None 4 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 279 9 2 4 1.4 CC(=O)NCCN(C)c1cccc(OCCCCN)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4214348 163927 0 None 4 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 279 9 2 4 1.4 CC(=O)NCCN(C)c1cccc(OCCCCN)c1 10.1021/acs.jmedchem.8b00893
44264705 202746 1 None -79 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 284 6 2 3 4.2 CCCC(=O)Nc1ccc(Nc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7229 202746 1 None -79 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 284 6 2 3 4.2 CCCC(=O)Nc1ccc(Nc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
127040022 137411 0 None -6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 410 5 1 4 5.5 COc1ccc2oc(-c3c4ccccc4cc4ccccc34)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3764063 137411 0 None -6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 410 5 1 4 5.5 COc1ccc2oc(-c3c4ccccc4cc4ccccc34)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
9819843 206387 0 None -20 2 Human 7.5 pKi = 7.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 351 8 1 3 4.3 COc1ccc2oc(CCCc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL98074 206387 0 None -20 2 Human 7.5 pKi = 7.5 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 351 8 1 3 4.3 COc1ccc2oc(CCCc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
145978811 163297 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 531 16 2 5 6.4 CC(=O)NCCN(C)c1cccc(OCCCCCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4206642 163297 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 531 16 2 5 6.4 CC(=O)NCCN(C)c1cccc(OCCCCCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
137655489 158417 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 245 4 2 3 1.5 COc1cnc2cccc(CCNC(N)=O)c2c1 10.1016/j.ejmech.2016.12.013
CHEMBL4096197 158417 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 245 4 2 3 1.5 COc1cnc2cccc(CCNC(N)=O)c2c1 10.1016/j.ejmech.2016.12.013
25022442 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1016/j.bmc.2009.04.068
CHEMBL514413 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1016/j.bmc.2009.04.068
11058163 206463 0 None -22 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 386 5 1 3 4.1 COc1cccc2c1c(Br)c(CNC(C)=O)n2Cc1ccccc1 10.1021/jm001125h
CHEMBL98520 206463 0 None -22 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 386 5 1 3 4.1 COc1cccc2c1c(Br)c(CNC(C)=O)n2Cc1ccccc1 10.1021/jm001125h
49865423 15767 2 None -4 2 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 4 1 2 2.3 CC(=O)NC(C)CSc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223345 15767 2 None -4 2 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 4 1 2 2.3 CC(=O)NC(C)CSc1ccccc1 10.1016/j.bmc.2010.06.100
25022442 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1016/j.bmc.2008.07.012
CHEMBL514413 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1016/j.bmc.2008.07.012
145982333 165993 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4279639 165993 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 3 2 2 2.8 CNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL3109563 209335 0 None -3 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 minsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 mins
ChEMBL None None None COc1ccc2c(c1)c(CCNC(C)=O)c1n2[B-](F)(F)[N+]2=C(C)C=C(C)C2=C1 10.1021/ml4004155
129776 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1016/j.ejmech.2019.111847
1364 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1016/j.ejmech.2019.111847
CHEMBL339105 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1016/j.ejmech.2019.111847
129776 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1021/jm401343c
1364 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1021/jm401343c
CHEMBL339105 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1021/jm401343c
71508235 86633 0 None -95 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 327 8 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1-c1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326203 86633 0 None -95 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 327 8 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1-c1cccc(OC)c1 10.1016/j.bmc.2012.10.060
25022442 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1021/jm800974d
CHEMBL514413 188958 0 None -5 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 375 4 1 4 3.3 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CC2Cc3ccccc3N2C1 10.1021/jm800974d
162649850 179548 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
CHEMBL4748822 179548 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1ncnc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
24750194 89504 0 None -87 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 324 7 1 3 3.8 COc1cccc(N(CCNC(=O)C2CCC2)c2ccccc2)c1 10.1021/jm700957j
CHEMBL238049 89504 0 None -87 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 324 7 1 3 3.8 COc1cccc(N(CCNC(=O)C2CCC2)c2ccccc2)c1 10.1021/jm700957j
122188353 122639 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 322 6 1 2 3.9 CCC(=O)NCCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612610 122639 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 322 6 1 2 3.9 CCC(=O)NCCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
20590664 123142 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 390 9 2 2 5.4 CCNC(=O)NC[C@@H]1C[C@H]1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL362097 123142 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 390 9 2 2 5.4 CCNC(=O)NC[C@@H]1C[C@H]1c1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
44429451 148668 0 None -15 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 352 6 1 3 3.4 CCCC(=O)NCCc1cn(C)c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL394406 148668 0 None -15 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 352 6 1 3 3.4 CCCC(=O)NCCc1cn(C)c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
11002150 107054 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 334 6 1 3 3.7 COc1cccc2c1cc(CCNC(=O)C1CC1)n2-c1ccccc1 10.1021/jm001125h
CHEMBL318871 107054 0 None -7 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 334 6 1 3 3.7 COc1cccc2c1cc(CCNC(=O)C1CC1)n2-c1ccccc1 10.1021/jm001125h
44349270 112580 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 286 6 1 3 3.4 CC(C)c1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL331317 112580 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 286 6 1 3 3.4 CC(C)c1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
44264843 203129 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 300 5 1 4 4.0 CCOC(=O)Nc1ccc(N(C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7556 203129 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 300 5 1 4 4.0 CCOC(=O)Nc1ccc(N(C)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
137640407 156190 0 None -67 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 270 5 1 3 2.5 COc1ccc2cccc(CCC(=O)NC3CC3)c2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4070527 156190 0 None -67 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 270 5 1 3 2.5 COc1ccc2cccc(CCC(=O)NC3CC3)c2n1 10.1016/j.ejmech.2016.12.013
11638009 165199 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 5 1 3 3.1 CCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCC1 10.1021/jm0512544
CHEMBL424693 165199 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 5 1 3 3.1 CCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCC1 10.1021/jm0512544
44587356 192771 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 423 8 3 5 2.8 COc1ccc2c(c1)CC(CO)N2Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1016/j.bmc.2008.07.012
CHEMBL525374 192771 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 423 8 3 5 2.8 COc1ccc2c(c1)CC(CO)N2Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1016/j.bmc.2008.07.012
168296374 191910 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
CHEMBL5209359 191910 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 505 9 1 8 4.5 CCN(CC)c1ccc2c(COC(=O)n3cc(CCNC(C)=O)c4cc(OC)ccc43)cc(=O)oc2c1 10.1021/acs.jmedchem.2c00717
145966403 163645 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 497 13 2 6 4.9 CC(=O)NCCN(C)c1cccc(OCCCCOc2cccc(OC(=O)NC3CCCCC3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4210884 163645 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 497 13 2 6 4.9 CC(=O)NCCN(C)c1cccc(OCCCCOc2cccc(OC(=O)NC3CCCCC3)c2)c1 10.1021/acs.jmedchem.8b00893
44349294 18352 1 None -5 2 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 323 6 2 3 3.7 CCNC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL127576 18352 1 None -5 2 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 323 6 2 3 3.7 CCNC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
23658143 155824 1 None -6 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
CHEMBL4066279 155824 1 None -6 2 Human 6.5 pKi = 6.5 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
49865375 15741 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OC[C@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223278 15741 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OC[C@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
127038131 136115 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 363 9 1 3 4.4 CC(=O)NCCc1cccc2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3740052 136115 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 363 9 1 3 4.4 CC(=O)NCCc1cccc2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
122178509 120801 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580919 120801 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1021/acs.jmedchem.5b00245
122178509 120801 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
CHEMBL3580919 120801 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 259 4 2 4 1.6 COc1ccc2[nH]cc(CCc3n[nH]c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
127038131 136115 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 363 9 1 3 4.4 CC(=O)NCCc1cccc2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3740052 136115 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 363 9 1 3 4.4 CC(=O)NCCc1cccc2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
49865373 15739 2 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OCC(C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223276 15739 2 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OCC(C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
44264861 203424 0 None -74 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 310 5 1 3 4.1 CCCC(=O)Nc1ccc(N(C)c2cccc3c2CCO3)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7807 203424 0 None -74 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 310 5 1 3 4.1 CCCC(=O)Nc1ccc(N(C)c2cccc3c2CCO3)cc1 10.1016/j.bmcl.2003.11.030
16094587 82835 3 None -72 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 297 7 1 2 3.7 CCC(=O)NCCC(c1ccccc1)c1cccc(OC)c1 10.1021/jm060850a
CHEMBL218774 82835 3 None -72 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 297 7 1 2 3.7 CCC(=O)NCCC(c1ccccc1)c1cccc(OC)c1 10.1021/jm060850a
16094592 82858 1 None -6 2 Human 5.4 pKi = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 251 4 1 1 3.4 CC(=O)NC/C(=C/c1ccccc1)c1ccccc1 10.1021/jm060850a
CHEMBL218926 82858 1 None -6 2 Human 5.4 pKi = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 251 4 1 1 3.4 CC(=O)NC/C(=C/c1ccccc1)c1ccccc1 10.1021/jm060850a
49865267 15685 2 None -7 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 225 5 1 3 1.9 COc1ccccc1SCCNC(C)=O 10.1016/j.bmc.2010.06.100
CHEMBL1223127 15685 2 None -7 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 225 5 1 3 1.9 COc1ccccc1SCCNC(C)=O 10.1016/j.bmc.2010.06.100
49865374 15740 0 None -7 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OC[C@@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223277 15740 0 None -7 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(OC[C@@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
122188235 122623 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 308 5 1 2 3.5 CCC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612467 122623 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 308 5 1 2 3.5 CCC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
145971692 162458 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 264 3 0 3 3.8 O=c1ccc2ccc(O/C=C/c3ccccc3)cc2o1 10.1021/acs.jnatprod.7b00853
CHEMBL4175759 162458 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 264 3 0 3 3.8 O=c1ccc2ccc(O/C=C/c3ccccc3)cc2o1 10.1021/acs.jnatprod.7b00853
16743125 91857 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 296 5 1 2 3.4 O=C(NCCCc1cn2c3c(cccc13)CCC2)C1CCC1 10.1016/j.ejmech.2007.01.005
CHEMBL242786 91857 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 296 5 1 2 3.4 O=C(NCCCc1cn2c3c(cccc13)CCC2)C1CCC1 10.1016/j.ejmech.2007.01.005
49865425 15769 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 4 1 2 2.3 CC(=O)N[C@@H](C)CSc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223347 15769 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 4 1 2 2.3 CC(=O)N[C@@H](C)CSc1ccccc1 10.1016/j.bmc.2010.06.100
4207624 15664 35 None -5 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1ccccc1OCCNC(C)=O 10.1016/j.bmc.2010.06.100
CHEMBL1223055 15664 35 None -5 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1ccccc1OCCNC(C)=O 10.1016/j.bmc.2010.06.100
46885230 8094 0 None -8 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 223 5 2 3 1.5 COc1ccc(O)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1092062 8094 0 None -8 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 223 5 2 3 1.5 COc1ccc(O)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
25210131 174733 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 7 2 3 3.8 CCC(=O)NCCc1c(CN2CCc3ccccc32)[nH]c2ccc(OC)cc12 10.1021/jm800974d
CHEMBL457352 174733 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 7 2 3 3.8 CCC(=O)NCCc1c(CN2CCc3ccccc32)[nH]c2ccc(OC)cc12 10.1021/jm800974d
25210131 174733 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 7 2 3 3.8 CCC(=O)NCCc1c(CN2CCc3ccccc32)[nH]c2ccc(OC)cc12 10.1021/jm800974d
CHEMBL457352 174733 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 7 2 3 3.8 CCC(=O)NCCc1c(CN2CCc3ccccc32)[nH]c2ccc(OC)cc12 10.1021/jm800974d
71508232 86631 0 None -524 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 351 7 1 3 3.6 CCC(=O)NCCCc1cc(OC)ccc1C#Cc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
CHEMBL2326200 86631 0 None -524 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 351 7 1 3 3.6 CCC(=O)NCCCc1cc(OC)ccc1C#Cc1cccc(OC)c1 10.1016/j.bmc.2012.10.060
44579296 186202 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 376 6 2 3 4.2 COc1ccc2cc(-c3cccc(NC(C)=O)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL489170 186202 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 376 6 2 3 4.2 COc1ccc2cc(-c3cccc(NC(C)=O)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
145969866 164278 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 546 15 3 6 4.8 CC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4218897 164278 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 546 15 3 6 4.8 CC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)c1 10.1021/acs.jmedchem.8b00893
56662798 64109 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 554 21 2 6 5.4 COc1cccc(N(CCCCCCCCCCN(CCNC(C)=O)c2cccc(OC)c2)CCNC(C)=O)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813326 64109 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 554 21 2 6 5.4 COc1cccc(N(CCCCCCCCCCN(CCNC(C)=O)c2cccc(OC)c2)CCNC(C)=O)c1 10.1016/j.bmc.2011.06.063
10704742 106764 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1cccc2cc(CCNC(C)=O)[nH]c12 10.1021/jm001125h
CHEMBL316952 106764 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1cccc2cc(CCNC(C)=O)[nH]c12 10.1021/jm001125h
10704742 106764 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1cccc2cc(CCNC(C)=O)[nH]c12 10.1021/jm970721h
CHEMBL316952 106764 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1cccc2cc(CCNC(C)=O)[nH]c12 10.1021/jm970721h
13250272 15683 14 None -11 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 195 4 1 2 1.9 CC(=O)NCCSc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223125 15683 14 None -11 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 195 4 1 2 1.9 CC(=O)NCCSc1ccccc1 10.1016/j.bmc.2010.06.100
44579261 186386 0 None -87 2 Human 5.4 pKi = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 363 6 2 3 3.9 COc1ccc2cc(-c3cccc(C(=O)O)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL490594 186386 0 None -87 2 Human 5.4 pKi = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 363 6 2 3 3.9 COc1ccc2cc(-c3cccc(C(=O)O)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
44424026 141792 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 546 17 4 4 5.8 COc1ccc2[nH]cc(CCNC(=O)CCCCCCCCC(=O)NCCc3c[nH]c4ccc(OC)cc34)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL388591 141792 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 546 17 4 4 5.8 COc1ccc2[nH]cc(CCNC(=O)CCCCCCCCC(=O)NCCc3c[nH]c4ccc(OC)cc34)c2c1 10.1016/j.bmc.2007.03.080
10709646 206088 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 304 3 1 2 3.5 CC(=O)NCCc1c2n(c3ccccc13)CCc1ccccc1-2 10.1021/jm980684+
CHEMBL9634 206088 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 304 3 1 2 3.5 CC(=O)NCCc1c2n(c3ccccc13)CCc1ccccc1-2 10.1021/jm980684+
11219713 125309 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 279 3 1 1 3.4 CC(=O)NCCC1Cc2ccccc2Cc2ccccc21 10.1021/jm040768k
CHEMBL364835 125309 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 279 3 1 1 3.4 CC(=O)NCCC1Cc2ccccc2Cc2ccccc21 10.1021/jm040768k
16094579 80415 5 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 267 6 1 1 3.3 CCC(=O)NCCc1cccc(Cc2ccccc2)c1 10.1021/jm060850a
CHEMBL215252 80415 5 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 267 6 1 1 3.3 CCC(=O)NCCc1cccc(Cc2ccccc2)c1 10.1021/jm060850a
44394338 121516 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 405 8 2 3 4.9 CCNC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
CHEMBL359561 121516 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 405 8 2 3 4.9 CCNC(=O)N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1 10.1016/j.bmcl.2004.07.055
71508234 696 0 None -38 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 341 9 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1Cc1cccc(c1)OC 10.1016/j.bmc.2012.10.060
7924 696 0 None -38 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 341 9 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1Cc1cccc(c1)OC 10.1016/j.bmc.2012.10.060
CHEMBL2326202 696 0 None -38 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation methodDisplacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method
ChEMBL 341 9 1 3 3.8 CCC(=O)NCCCc1cc(OC)ccc1Cc1cccc(c1)OC 10.1016/j.bmc.2012.10.060
10638747 206616 0 None -11 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 310 4 2 2 2.6 COc1ccc2c(Br)c(CCNC(C)=O)[nH]c2c1 10.1021/jm001125h
CHEMBL99512 206616 0 None -11 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 310 4 2 2 2.6 COc1ccc2c(Br)c(CCNC(C)=O)[nH]c2c1 10.1021/jm001125h
10638747 206616 0 None -11 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 310 4 2 2 2.6 COc1ccc2c(Br)c(CCNC(C)=O)[nH]c2c1 10.1021/jm970721h
CHEMBL99512 206616 0 None -11 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 310 4 2 2 2.6 COc1ccc2c(Br)c(CCNC(C)=O)[nH]c2c1 10.1021/jm970721h
44389839 64255 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 379 10 1 2 5.1 CC(C)C(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL181687 64255 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 379 10 1 2 5.1 CC(C)C(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
12071674 123412 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 351 9 1 2 4.5 CC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL362849 123412 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 351 9 1 2 4.5 CC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
145979282 166111 0 None -16 3 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4281915 166111 0 None -16 3 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
145988801 166482 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 283 4 1 2 3.4 COc1ccc2ccc3c(c2c1)C(CCNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4288925 166482 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 283 4 1 2 3.4 COc1ccc2ccc3c(c2c1)C(CCNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
145986700 166655 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 328 4 2 2 3.5 CCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4292109 166655 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 328 4 2 2 3.5 CCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137650826 156951 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 289 5 2 3 2.3 CCNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4079699 156951 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 289 5 2 3 2.3 CCNC(=S)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
46888491 8568 0 None 20 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 501 13 3 4 4.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4[nH]cc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095522 8568 0 None 20 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 501 13 3 4 4.9 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4[nH]cc(CCNC(C)=O)c4c3)cc12 10.1016/j.bmc.2010.04.008
10522675 4257 0 None -20 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 6 1 3 4.3 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCc1ccccc1-2 10.1021/jm980684+
CHEMBL10099 4257 0 None -20 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 6 1 3 4.3 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCc1ccccc1-2 10.1021/jm980684+
10522675 4257 0 None -20 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 362 6 1 3 4.3 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCc1ccccc1-2 10.1016/j.ejmech.2019.111847
CHEMBL10099 4257 0 None -20 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assayDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay
ChEMBL 362 6 1 3 4.3 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCc1ccccc1-2 10.1016/j.ejmech.2019.111847
16656789 88109 0 None -63 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1cccc(N(CCNC(C)=O)c2ccccc2)c1 10.1021/jm700957j
CHEMBL235327 88109 0 None -63 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1cccc(N(CCNC(C)=O)c2ccccc2)c1 10.1021/jm700957j
24750071 98450 0 None -39 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 312 8 1 3 3.8 CCCC(=O)NCCN(c1ccccc1)c1cccc(OC)c1 10.1021/jm700957j
CHEMBL279401 98450 0 None -39 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 312 8 1 3 3.8 CCCC(=O)NCCN(c1ccccc1)c1cccc(OC)c1 10.1021/jm700957j
44429448 87305 0 None -7 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 324 5 2 2 3.0 CCC(=O)NCCc1c[nH]c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL233729 87305 0 None -7 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 324 5 2 2 3.0 CCC(=O)NCCc1c[nH]c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
49865319 15705 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 251 7 1 3 2.4 CCCC(=O)NCC(C)Oc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223193 15705 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 251 7 1 3 2.4 CCCC(=O)NCC(C)Oc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
10704399 21292 0 None -8 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 225 2 1 1 2.6 CC(=O)NCC1Cc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL131602 21292 0 None -8 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 225 2 1 1 2.6 CC(=O)NCC1Cc2cccc3cccc1c23 10.1021/jm000922c
11652196 137772 0 None -9 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 288 6 1 3 3.2 CCCC(=O)NCC(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
CHEMBL377101 137772 0 None -9 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 288 6 1 3 3.2 CCCC(=O)NCC(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
10495702 203514 0 None -3 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 317 8 2 4 2.3 CCC(=O)NCCc1c(OCCO)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
CHEMBL78751 203514 0 None -3 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 317 8 2 4 2.3 CCC(=O)NCCc1c(OCCO)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
10729569 116043 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 253 4 1 1 3.4 CCC(=O)NCCC1Cc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL336333 116043 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 253 4 1 1 3.4 CCC(=O)NCCC1Cc2cccc3cccc1c23 10.1021/jm000922c
9840647 97756 0 None -25 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 334 5 1 3 3.7 CCC(=O)NCCc1c2n(c3ccc(OC)cc13)Cc1ccccc1-2 10.1021/jm980684+
CHEMBL274317 97756 0 None -25 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 334 5 1 3 3.7 CCC(=O)NCCc1c2n(c3ccc(OC)cc13)Cc1ccccc1-2 10.1021/jm980684+
44358276 118454 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 289 4 2 3 1.9 CCCNC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL342393 118454 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 289 4 2 3 1.9 CCCNC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
57781240 185396 0 None -36 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 334 5 1 3 4.0 CC(=O)NCCC1CCc2ccc3nc(Cc4ccccc4)oc3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4870108 185396 0 None -36 2 Human 8.4 pKi = 8.4 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 334 5 1 3 4.0 CC(=O)NCCC1CCc2ccc3nc(Cc4ccccc4)oc3c21 10.1021/acs.jmedchem.0c01836
1350 1951 0 None -95 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10.1021/jm980684+
4172142 1951 0 None -95 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10.1021/jm980684+
CHEMBL10009 1951 0 None -95 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10.1021/jm980684+
1350 1951 0 None -95 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10.1021/jm401343c
4172142 1951 0 None -95 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10.1021/jm401343c
CHEMBL10009 1951 0 None -95 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10.1021/jm401343c
44348996 17010 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 272 6 1 3 2.8 CCc1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL125642 17010 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 272 6 1 3 2.8 CCc1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
127029516 137096 0 None -6 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3occ(CNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3758225 137096 0 None -6 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 269 3 1 3 3.2 COc1ccc2ccc3occ(CNC(C)=O)c3c2c1 10.1016/j.ejmech.2015.12.047
23642307 158337 1 None -8 3 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc(C(CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
CHEMBL4095334 158337 1 None -8 3 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc(C(CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
145976009 162968 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 541 15 3 4 7.0 CC(=O)NCCc1c[nH]c2ccc(OCCCCCCCCNC(=O)Oc3cccc(-c4ccccc4)c3)cc12 10.1021/acs.jmedchem.8b00893
CHEMBL4202816 162968 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 541 15 3 4 7.0 CC(=O)NCCc1c[nH]c2ccc(OCCCCCCCCNC(=O)Oc3cccc(-c4ccccc4)c3)cc12 10.1021/acs.jmedchem.8b00893
44272334 67278 0 None -17 2 Human 8.3 pKi = 8.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 6 2 3 3.5 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C(C)C)c2O1 10.1016/j.bmcl.2003.12.052
CHEMBL19050 67278 0 None -17 2 Human 8.3 pKi = 8.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 302 6 2 3 3.5 CCCC1Nc2cccc([C@@H]3C[C@H]3CNC(=O)C(C)C)c2O1 10.1016/j.bmcl.2003.12.052
44272430 166368 0 None -15 2 Human 8.3 pKi = 8.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 288 5 2 3 3.1 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
CHEMBL428692 166368 0 None -15 2 Human 8.3 pKi = 8.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 288 5 2 3 3.1 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
11550834 139001 0 None -4 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 5 1 3 2.8 CCC(=O)NCC(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
CHEMBL379616 139001 0 None -4 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 274 5 1 3 2.8 CCC(=O)NCC(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
22718555 16397 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 6 1 3 3.7 CC(C)C(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL123973 16397 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 6 1 3 3.7 CC(C)C(=O)NCCCc1cccc2nc(C(C)C)oc12 10.1016/j.bmcl.2004.04.082
22718530 17750 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 294 5 1 3 3.6 CC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL126005 17750 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 294 5 1 3 3.6 CC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
19703063 28687 1 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1016/j.bmcl.2011.02.097
CHEMBL137969 28687 1 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1016/j.bmcl.2011.02.097
19703063 28687 1 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1016/j.ejmech.2016.01.008
CHEMBL137969 28687 1 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1016/j.ejmech.2016.01.008
1347 162 51 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10.1016/j.ejmech.2019.111847
1864 162 51 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10.1016/j.ejmech.2019.111847
CHEMBL127421 162 51 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10.1016/j.ejmech.2019.111847
1353 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
9998187 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
CHEMBL33549 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
1353 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm401343c
9998187 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm401343c
CHEMBL33549 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm401343c
25209861 174637 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 8 2 3 4.6 CCCC(=O)NCCc1c(CN2c3ccccc3CC2C)[nH]c2ccc(OC)cc12 10.1021/jm800974d
CHEMBL457138 174637 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 8 2 3 4.6 CCCC(=O)NCCc1c(CN2c3ccccc3CC2C)[nH]c2ccc(OC)cc12 10.1021/jm800974d
25210133 188960 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.7 COc1ccc2[nH]c(CN3CCc4cc(C)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL514427 188960 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.7 COc1ccc2[nH]c(CN3CCc4cc(C)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
44436051 150819 6 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1cccc(OCCNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL396132 150819 6 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1cccc(OCCNC(C)=O)c1 10.1016/j.bmc.2010.06.100
1353 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm048956y
9998187 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm048956y
CHEMBL33549 3368 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm048956y
46885285 8068 0 None -186 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 265 8 1 3 2.6 CCCOc1ccc(OC)cc1CCCNC(C)=O 10.1016/j.bmcl.2010.02.084
CHEMBL1091894 8068 0 None -186 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 265 8 1 3 2.6 CCCOc1ccc(OC)cc1CCCNC(C)=O 10.1016/j.bmcl.2010.02.084
10657206 119171 2 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 2.2 CCC(=O)NCc1cc2c(OC)cccc2[nH]1 10.1021/jm001125h
CHEMBL34728 119171 2 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 2.2 CCC(=O)NCc1cc2c(OC)cccc2[nH]1 10.1021/jm001125h
10657206 119171 2 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 2.2 CCC(=O)NCc1cc2c(OC)cccc2[nH]1 10.1021/jm970721h
CHEMBL34728 119171 2 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 2.2 CCC(=O)NCc1cc2c(OC)cccc2[nH]1 10.1021/jm970721h
44264904 203899 0 None -57 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 295 5 1 2 4.0 CCCC(=O)Nc1ccc(Cc2cccc3c2CCO3)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL8169 203899 0 None -57 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 295 5 1 2 4.0 CCCC(=O)Nc1ccc(Cc2cccc3c2CCO3)cc1 10.1016/j.bmcl.2003.11.030
25209861 174637 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 8 2 3 4.6 CCCC(=O)NCCc1c(CN2c3ccccc3CC2C)[nH]c2ccc(OC)cc12 10.1021/jm800974d
CHEMBL457138 174637 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 405 8 2 3 4.6 CCCC(=O)NCCc1c(CN2c3ccccc3CC2C)[nH]c2ccc(OC)cc12 10.1021/jm800974d
25210133 188960 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.7 COc1ccc2[nH]c(CN3CCc4cc(C)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL514427 188960 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 6 2 3 3.7 COc1ccc2[nH]c(CN3CCc4cc(C)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
16743295 92743 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 284 6 1 2 3.4 CCCC(=O)NCCCc1cn2c3c(cccc13)CCC2 10.1016/j.ejmech.2007.01.005
CHEMBL244472 92743 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 284 6 1 2 3.4 CCCC(=O)NCCCc1cn2c3c(cccc13)CCC2 10.1016/j.ejmech.2007.01.005
5151463 82906 12 None -29 2 Human 5.4 pKi = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 253 5 1 1 3.3 CC(=O)NCCC(c1ccccc1)c1ccccc1 10.1021/jm060850a
CHEMBL219177 82906 12 None -29 2 Human 5.4 pKi = 5.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 253 5 1 1 3.3 CC(=O)NCCC(c1ccccc1)c1ccccc1 10.1021/jm060850a
10545399 203791 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 344 9 1 4 2.9 CCC(=O)NCCc1c(OCCN(C)C)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
CHEMBL80792 203791 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 344 9 1 4 2.9 CCC(=O)NCCc1c(OCCN(C)C)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
44394556 123693 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 402 8 1 3 5.1 O=C(N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1)C1CC1 10.1016/j.bmcl.2004.07.055
CHEMBL363441 123693 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 402 8 1 3 5.1 O=C(N[C@H]1CCN(c2cccc3oc(CCCCc4ccccc4)cc23)C1)C1CC1 10.1016/j.bmcl.2004.07.055
56661512 64101 0 None 23 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 470 15 2 6 3.1 CC(=O)NCCN(C)c1cccc(OCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813319 64101 0 None 23 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 470 15 2 6 3.1 CC(=O)NCCN(C)c1cccc(OCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
10959837 205834 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 379 10 1 3 5.3 CCCCCOc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL94919 205834 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 379 10 1 3 5.3 CCCCCOc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
49865147 15639 2 None -3 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1ccc(OC(C)CNC(C)=O)cc1 10.1016/j.bmc.2010.06.100
CHEMBL1222983 15639 2 None -3 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1ccc(OC(C)CNC(C)=O)cc1 10.1016/j.bmc.2010.06.100
127025788 137229 0 None -53 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 300 3 2 3 3.2 CNC(=S)NCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
CHEMBL3759372 137229 0 None -53 2 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 300 3 2 3 3.2 CNC(=S)NCc1cc2c(ccc3ccc(OC)cc32)o1 10.1016/j.ejmech.2015.12.047
130400672 156442 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 204 2 2 2 1.4 CC(=O)NCC1CNc2ccccc2C1 10.1021/acs.jmedchem.8b00359
CHEMBL4073210 156442 0 None -3 2 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 204 2 2 2 1.4 CC(=O)NCC1CNc2ccccc2C1 10.1021/acs.jmedchem.8b00359
10595585 98081 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 374 5 1 3 4.3 COc1ccc2c(c1)c(CCNC(=O)C1CCC1)c1n2CCc2ccccc2-1 10.1021/jm980684+
CHEMBL276490 98081 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 374 5 1 3 4.3 COc1ccc2c(c1)c(CCNC(=O)C1CCC1)c1n2CCc2ccccc2-1 10.1021/jm980684+
44349362 16382 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 286 7 1 3 3.2 CCCc1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL123899 16382 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 286 7 1 3 3.2 CCCc1nc2cccc(CCCNC(=O)C3CC3)c2o1 10.1016/j.bmcl.2004.04.082
46884553 8198 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 343 9 1 4 3.4 COc1cccc(COc2ccc(OC)cc2CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1092646 8198 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 343 9 1 4 3.4 COc1cccc(COc2ccc(OC)cc2CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
910172 37481 23 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 252 3 0 3 3.4 O=c1ccc2ccc(OCc3ccccc3)cc2o1 10.1021/acs.jnatprod.7b00853
CHEMBL145781 37481 23 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 252 3 0 3 3.4 O=c1ccc2ccc(OCc3ccccc3)cc2o1 10.1021/acs.jnatprod.7b00853
145965883 163519 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 307 11 2 4 2.2 CC(=O)NCCN(C)c1cccc(OCCCCCCN)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4209446 163519 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 307 11 2 4 2.2 CC(=O)NCCN(C)c1cccc(OCCCCCCN)c1 10.1021/acs.jmedchem.8b00893
122188236 122624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.1 CC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612468 122624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.1 CC(=O)NCC1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
122188237 122625 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.1 CC(=O)NC[C@H]1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
CHEMBL3612469 122625 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 294 4 1 2 3.1 CC(=O)NC[C@H]1CCc2ccccc2N1Cc1ccccc1 10.1021/acs.jmedchem.5b01066
10712600 4277 0 None -48 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 346 5 1 3 3.7 COc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2Cc2ccccc2-1 10.1021/jm980684+
CHEMBL10110 4277 0 None -48 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 346 5 1 3 3.7 COc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2Cc2ccccc2-1 10.1021/jm980684+
11602301 76333 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 326 5 1 3 3.5 COc1ccc2c(c1)c(C1(CNC(=O)C3CC3)CCCC1)cn2C 10.1021/jm0512544
CHEMBL206471 76333 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 326 5 1 3 3.5 COc1ccc2c(c1)c(C1(CNC(=O)C3CC3)CCCC1)cn2C 10.1021/jm0512544
10950593 111020 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 459 6 1 3 5.7 COc1ccc2oc(Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL327864 111020 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 459 6 1 3 5.7 COc1ccc2oc(Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
164946945 189625 1 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5174929 189625 1 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 427 9 1 7 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2Cc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
49865378 15744 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SC[C@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223281 15744 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(SC[C@H](C)NC(C)=O)c1 10.1016/j.bmc.2010.06.100
11501012 76874 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 340 5 1 3 3.9 COc1ccc2c(c1)c(C1(CNC(=O)C3CCC3)CCCC1)cn2C 10.1021/jm0512544
CHEMBL207959 76874 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 340 5 1 3 3.9 COc1ccc2c(c1)c(C1(CNC(=O)C3CCC3)CCCC1)cn2C 10.1021/jm0512544
49865203 15658 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(O[C@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223049 15658 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 223 5 1 3 1.6 COc1cccc(O[C@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
122188226 122615 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 263 4 3 3 1.7 CCNC(=O)NCC1CCc2c(cccc2OC)N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612457 122615 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 263 4 3 3 1.7 CCNC(=O)NCC1CCc2c(cccc2OC)N1 10.1021/acs.jmedchem.5b01066
11616210 138915 0 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 4 1 3 2.7 COc1ccc2c(c1)c(C1(CNC(C)=O)CCC1)cn2C 10.1021/jm0512544
CHEMBL379413 138915 0 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 4 1 3 2.7 COc1ccc2c(c1)c(C1(CNC(C)=O)CCC1)cn2C 10.1021/jm0512544
44347098 16224 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 344 5 1 4 2.7 CCCCC(=O)n1c(OC)cc2c1=C(CN)C1CCCCC(C)C1C=2 10.1021/jm970721h
CHEMBL123119 16224 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 344 5 1 4 2.7 CCCCC(=O)n1c(OC)cc2c1=C(CN)C1CCCCC(C)C1C=2 10.1021/jm970721h
CHEMBL3109561 209333 0 None 6 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 minsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 mins
ChEMBL None None None COc1ccc(C2=[N+]3C(=Cc4c(CCNC(C)=O)c5cc(OC)ccc5n4[B-]3(F)F)C=C2)cc1 10.1021/ml4004155
11065731 101398 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 277 5 2 4 1.8 COc1cc([N+](=O)[O-])c2[nH]cc(CCNC(C)=O)c2c1 10.1021/jm011053+
CHEMBL300729 101398 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 277 5 2 4 1.8 COc1cc([N+](=O)[O-])c2[nH]cc(CCNC(C)=O)c2c1 10.1021/jm011053+
44358035 29735 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 260 3 1 3 1.7 CCC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL138848 29735 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 260 3 1 3 1.7 CCC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
44579163 181537 0 None -53 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 362 6 1 3 4.3 COc1ccc2cc(-c3cccc(N(C)C)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL478217 181537 0 None -53 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 362 6 1 3 4.3 COc1ccc2cc(-c3cccc(N(C)C)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
44349329 18347 1 None -13 2 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 289 7 2 3 3.0 CCCc1nc2cccc(CCCNC(=O)NCC)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL127565 18347 1 None -13 2 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 289 7 2 3 3.0 CCCc1nc2cccc(CCCNC(=O)NCC)c2o1 10.1016/j.bmcl.2004.04.082
11500596 138137 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 312 5 2 2 3.5 COc1ccc2[nH]cc(C3(CNC(=O)C4CCC4)CCC3)c2c1 10.1021/jm0512544
CHEMBL377809 138137 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 312 5 2 2 3.5 COc1ccc2[nH]cc(C3(CNC(=O)C4CCC4)CCC3)c2c1 10.1021/jm0512544
122188230 122618 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 277 4 2 3 1.8 CCNC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612461 122618 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 277 4 2 3 1.8 CCNC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
10424693 109142 1 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 297 4 1 2 3.1 COc1ccc2cccc(CCNC(=O)C(F)(F)F)c2c1 10.1039/C5MD00190K
CHEMBL322339 109142 1 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 297 4 1 2 3.1 COc1ccc2cccc(CCNC(=O)C(F)(F)F)c2c1 10.1039/C5MD00190K
127038129 136336 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 311 5 1 2 3.3 COc1ccc2cccc(CCNC(=O)C(Cl)Cl)c2c1 10.1039/C5MD00190K
CHEMBL3742090 136336 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 311 5 1 2 3.3 COc1ccc2cccc(CCNC(=O)C(Cl)Cl)c2c1 10.1039/C5MD00190K
86273226 120791 0 None -5 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 256 5 2 2 1.9 C#CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
CHEMBL3580908 120791 0 None -5 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 256 5 2 2 1.9 C#CCNC(=O)CCc1c[nH]c2ccc(OC)cc12 10.1021/acs.jmedchem.5b00245
145983929 165857 0 None -6 3 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 4 1 3 2.8 COc1ccc2ccc3c(c2n1)C(CCNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4277185 165857 0 None -6 3 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 284 4 1 3 2.8 COc1ccc2ccc3c(c2n1)C(CCNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
145993566 166806 0 None -25 3 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 312 5 2 2 3.6 CCCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4294790 166806 0 None -25 3 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 312 5 2 2 3.6 CCCNC(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137642160 157835 0 None -165 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 308 5 1 5 1.3 COc1ccc2cccc(CCC(=O)NS(C)(=O)=O)c2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4089965 157835 0 None -165 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 308 5 1 5 1.3 COc1ccc2cccc(CCC(=O)NS(C)(=O)=O)c2n1 10.1016/j.ejmech.2016.12.013
127038129 136336 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 311 5 1 2 3.3 COc1ccc2cccc(CCNC(=O)C(Cl)Cl)c2c1 10.1039/C5MD00190K
CHEMBL3742090 136336 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 311 5 1 2 3.3 COc1ccc2cccc(CCNC(=O)C(Cl)Cl)c2c1 10.1039/C5MD00190K
44272431 98388 0 None -4 2 Human 8.3 pKi = 8.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 274 4 2 3 2.7 CC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
CHEMBL278922 98388 0 None -4 2 Human 8.3 pKi = 8.3 Binding
Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1ABinding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 274 4 2 3 2.7 CC(=O)NC[C@@H]1C[C@H]1c1cccc2c1OC(C(C)C)N2 10.1016/j.bmcl.2003.12.052
16750569 86920 0 None -14 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 338 6 2 2 3.4 CCCC(=O)NCCc1c[nH]c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL233308 86920 0 None -14 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 338 6 2 2 3.4 CCCC(=O)NCCc1c[nH]c2c(Br)cc(OC)cc12 10.1016/j.bmc.2007.04.013
9888609 8789 0 None 46 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO-K1 cells after 2 hrsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO-K1 cells after 2 hrs
ChEMBL 424 7 2 2 5.0 CC(=O)NCCc1cccc2ccc(-c3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1039/C5MD00190K
CHEMBL1097525 8789 0 None 46 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO-K1 cells after 2 hrsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO-K1 cells after 2 hrs
ChEMBL 424 7 2 2 5.0 CC(=O)NCCc1cccc2ccc(-c3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1039/C5MD00190K
9888609 8789 0 None 46 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 424 7 2 2 5.0 CC(=O)NCCc1cccc2ccc(-c3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm401343c
CHEMBL1097525 8789 0 None 46 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 424 7 2 2 5.0 CC(=O)NCCc1cccc2ccc(-c3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm401343c
24750070 153007 4 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 208 5 2 3 1.2 COc1cccc(NCCNC(C)=O)c1 10.1021/jm700957j
CHEMBL398017 153007 4 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 208 5 2 3 1.2 COc1cccc(NCCNC(C)=O)c1 10.1021/jm700957j
122188231 122619 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 247 3 2 2 1.8 CCNC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
CHEMBL3612462 122619 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 247 3 2 2 1.8 CCNC(=O)NCC1CCc2ccccc2N1C 10.1021/acs.jmedchem.5b01066
10882307 205731 0 None -15 2 Human 8.3 pKi = 8.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 338 6 2 3 3.5 CNC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL94301 205731 0 None -15 2 Human 8.3 pKi = 8.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 338 6 2 3 3.5 CNC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
49865318 15704 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 265 6 1 3 2.7 COc1cccc(S[C@@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223192 15704 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 265 6 1 3 2.7 COc1cccc(S[C@@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
11644612 77880 0 None -9 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.4 COc1ccc2c(c1)c(C(C)CNC(C)=O)cn2C 10.1021/jm0512544
CHEMBL210791 77880 0 None -9 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.4 COc1ccc2c(c1)c(C(C)CNC(C)=O)cn2C 10.1021/jm0512544
90666306 108882 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 7 2 3 3.8 CCC(=O)NCCc1c(CN2Cc3ccccc3C2)[nH]c2ccc(OC)cc12 10.1039/C1MD00149C
CHEMBL3219327 108882 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 377 7 2 3 3.8 CCC(=O)NCCc1c(CN2Cc3ccccc3C2)[nH]c2ccc(OC)cc12 10.1039/C1MD00149C
127025784 137195 0 None -8 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3oc(CNC(=O)CF)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759084 137195 0 None -8 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3oc(CNC(=O)CF)cc3c2c1 10.1016/j.ejmech.2015.12.047
10424693 109142 1 None -2 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 297 4 1 2 3.1 COc1ccc2cccc(CCNC(=O)C(F)(F)F)c2c1 10.1039/C5MD00190K
CHEMBL322339 109142 1 None -2 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 297 4 1 2 3.1 COc1ccc2cccc(CCNC(=O)C(F)(F)F)c2c1 10.1039/C5MD00190K
25209998 189140 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 393 7 2 4 3.4 COc1ccc2c(c1)CCN2Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1021/jm800974d
CHEMBL515856 189140 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 393 7 2 4 3.4 COc1ccc2c(c1)CCN2Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1021/jm800974d
49865206 15662 1 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(S[C@@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223053 15662 1 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 239 5 1 3 2.3 COc1cccc(S[C@@H](C)CNC(C)=O)c1 10.1016/j.bmc.2010.06.100
122188349 122636 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 246 4 1 2 2.4 CCCN1c2ccccc2CCC1CNC(C)=O 10.1021/acs.jmedchem.5b01066
CHEMBL3612606 122636 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 246 4 1 2 2.4 CCCN1c2ccccc2CCC1CNC(C)=O 10.1021/acs.jmedchem.5b01066
25209998 189140 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 393 7 2 4 3.4 COc1ccc2c(c1)CCN2Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1021/jm800974d
CHEMBL515856 189140 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 393 7 2 4 3.4 COc1ccc2c(c1)CCN2Cc1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1021/jm800974d
23658144 157622 1 None -6 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
CHEMBL4087633 157622 1 None -6 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc([C@@H](CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
10712733 206690 0 None -48 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 5 1 3 3.9 CCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCc1ccccc1-2 10.1021/jm980684+
CHEMBL9997 206690 0 None -48 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 348 5 1 3 3.9 CCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCc1ccccc1-2 10.1021/jm980684+
10399579 202276 0 None -4 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 244 4 1 3 1.9 COc1ccc2nccc(CCNC(C)=O)c2c1 10.1016/S0960-894X(97)00392-2
CHEMBL69521 202276 0 None -4 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 244 4 1 3 1.9 COc1ccc2nccc(CCNC(C)=O)c2c1 10.1016/S0960-894X(97)00392-2
12985489 189632 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 349 6 2 3 3.7 COc1ccc2cc(-c3ccccc3CO)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL517502 189632 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 349 6 2 3 3.7 COc1ccc2cc(-c3ccccc3CO)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
44349258 16721 1 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 261 5 2 3 2.4 CCNC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL125226 16721 1 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 261 5 2 3 2.4 CCNC(=O)NCCCc1cccc2nc(C)oc12 10.1016/j.bmcl.2004.04.082
10903463 206613 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 324 5 2 2 3.0 CCC(=O)NCCc1[nH]c2cccc(OC)c2c1Br 10.1021/jm001125h
CHEMBL99502 206613 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 324 5 2 2 3.0 CCC(=O)NCCc1[nH]c2cccc(OC)c2c1Br 10.1021/jm001125h
24750069 149938 0 None -66 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 298 7 1 3 2.8 COc1cccc(N(CCNC(C)=O)Cc2ccccc2)c1 10.1021/jm700957j
CHEMBL395437 149938 0 None -66 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 298 7 1 3 2.8 COc1cccc(N(CCNC(C)=O)Cc2ccccc2)c1 10.1021/jm700957j
12985491 186387 0 None -91 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 411 6 1 2 5.1 COc1ccc2cc(-c3cccc(CBr)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL490595 186387 0 None -91 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 411 6 1 2 5.1 COc1ccc2cc(-c3cccc(CBr)c3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
118712359 113638 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 350 3 1 4 3.4 O=C(CN1CCCC2Cc3cc4c(cc3C21)OCO4)Nc1ccccc1 10.1016/j.ejmech.2014.09.038
CHEMBL3329376 113638 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 350 3 1 4 3.4 O=C(CN1CCCC2Cc3cc4c(cc3C21)OCO4)Nc1ccccc1 10.1016/j.ejmech.2014.09.038
162649247 179485 0 None -10 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 351 6 1 5 3.0 COc1cccc(-c2nc(CCNC(C)=O)c3cc(OC)ccc3n2)c1 10.1016/j.ejmech.2020.112078
CHEMBL4747996 179485 0 None -10 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 351 6 1 5 3.0 COc1cccc(-c2nc(CCNC(C)=O)c3cc(OC)ccc3n2)c1 10.1016/j.ejmech.2020.112078
10738183 4296 0 None -41 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 374 5 1 3 4.3 COc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2CCCc2ccccc2-1 10.1021/jm980684+
CHEMBL10124 4296 0 None -41 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 374 5 1 3 4.3 COc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2CCCc2ccccc2-1 10.1021/jm980684+
1358 124 35 None -870 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm401343c
3976006 124 35 None -870 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm401343c
CHEMBL285718 124 35 None -870 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm401343c
22718661 16645 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 7 1 3 3.2 CCCc1nc2cccc(CCCNC(=O)CC)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL124783 16645 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 7 1 3 3.2 CCCc1nc2cccc(CCCNC(=O)CC)c2o1 10.1016/j.bmcl.2004.04.082
168288029 191015 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 471 9 1 9 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5195595 191015 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes under dark condition by radioligand based competition binding assay
ChEMBL 471 9 1 9 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
54582194 60418 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 330 6 1 5 2.2 COc1ccc2c(CN3CCCCC3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760950 60418 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 330 6 1 5 2.2 COc1ccc2c(CN3CCCCC3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
16094582 82887 5 None -44 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 251 4 1 1 3.3 CC(=O)NCC=C(c1ccccc1)c1ccccc1 10.1021/jm060850a
CHEMBL219076 82887 5 None -44 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 251 4 1 1 3.3 CC(=O)NCC=C(c1ccccc1)c1ccccc1 10.1021/jm060850a
10666373 97856 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 5 1 3 4.3 CCOc1ccc2c(c1)c(CCNC(C)=O)c1n2CCCc2ccccc2-1 10.1021/jm980684+
CHEMBL274995 97856 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 5 1 3 4.3 CCOc1ccc2c(c1)c(CCNC(C)=O)c1n2CCCc2ccccc2-1 10.1021/jm980684+
10737372 4549 0 None -37 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 5 1 3 4.3 CCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCCc1ccccc1-2 10.1021/jm980684+
CHEMBL10293 4549 0 None -37 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 5 1 3 4.3 CCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCCc1ccccc1-2 10.1021/jm980684+
52953165 62064 0 None -218 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 389 7 1 3 5.6 C=CCC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779810 62064 0 None -218 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 389 7 1 3 5.6 C=CCC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
320362 49444 42 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 230 3 0 3 3.1 CC(C)=CCOc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
CHEMBL156692 49444 42 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 230 3 0 3 3.1 CC(C)=CCOc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
10563168 119174 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 258 4 2 2 2.6 COc1cccc2[nH]c(CNC(=O)C3CCC3)cc12 10.1021/jm001125h
CHEMBL34729 119174 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 258 4 2 2 2.6 COc1cccc2[nH]c(CNC(=O)C3CCC3)cc12 10.1021/jm001125h
10563168 119174 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 258 4 2 2 2.6 COc1cccc2[nH]c(CNC(=O)C3CCC3)cc12 10.1021/jm970721h
CHEMBL34729 119174 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 258 4 2 2 2.6 COc1cccc2[nH]c(CNC(=O)C3CCC3)cc12 10.1021/jm970721h
16094577 83051 4 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 297 7 1 2 3.5 CCC(=O)NCC(Cc1ccccc1)c1cccc(OC)c1 10.1021/jm060850a
CHEMBL220136 83051 4 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 297 7 1 2 3.5 CCC(=O)NCC(Cc1ccccc1)c1cccc(OC)c1 10.1021/jm060850a
9818487 172951 0 None -141 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 319 5 1 2 4.2 COc1ccc2cc(-c3ccccc3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
CHEMBL453138 172951 0 None -141 2 Human 7.3 pKi = 7.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 319 5 1 2 4.2 COc1ccc2cc(-c3ccccc3)cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.08.052
9884156 206130 0 None -77 2 Human 7.3 pKi = 7.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 335 7 1 3 3.9 C=CC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL96548 206130 0 None -77 2 Human 7.3 pKi = 7.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 335 7 1 3 3.9 C=CC(=O)NCCc1c(Cc2ccccc2)oc2ccc(OC)cc12 10.1021/jm0005252
44429457 168774 0 None -6 2 Human 5.3 pKi = 5.3 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 350 7 1 3 4.3 CCCC(=O)NCCc1cn(C)c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL441916 168774 0 None -6 2 Human 5.3 pKi = 5.3 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 350 7 1 3 4.3 CCCC(=O)NCCc1cn(C)c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
49865265 15682 2 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 225 5 1 3 1.9 COc1cccc(SCCNC(C)=O)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223124 15682 2 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 225 5 1 3 1.9 COc1cccc(SCCNC(C)=O)c1 10.1016/j.bmc.2010.06.100
162643514 181095 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 271 5 1 4 1.7 COc1ccc2ncnc(CCNC(=O)C3CC3)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4776540 181095 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 271 5 1 4 1.7 COc1ccc2ncnc(CCNC(=O)C3CC3)c2c1 10.1016/j.ejmech.2020.112078
11208632 122377 1 None -2 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 294 4 1 2 3.5 CCC(=O)NCCN1c2ccccc2CCc2ccccc21 10.1021/jm040768k
CHEMBL360600 122377 1 None -2 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 294 4 1 2 3.5 CCC(=O)NCCN1c2ccccc2CCc2ccccc21 10.1021/jm040768k
11277044 126068 1 None -6 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 263 2 1 1 3.3 CC(=O)NCC1=Cc2ccccc2Cc2ccccc21 10.1021/jm040768k
CHEMBL365249 126068 1 None -6 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 263 2 1 1 3.3 CC(=O)NCC1=Cc2ccccc2Cc2ccccc21 10.1021/jm040768k
16094588 136186 4 None -208 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 311 8 1 2 4.1 CCCC(=O)NCCC(c1ccccc1)c1cccc(OC)c1 10.1021/jm060850a
CHEMBL374075 136186 4 None -208 2 Human 6.3 pKi = 6.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 311 8 1 2 4.1 CCCC(=O)NCCC(c1ccccc1)c1cccc(OC)c1 10.1021/jm060850a
11046748 206189 0 None -19 2 Human 7.3 pKi = 7.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 365 8 1 4 3.9 C=CC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm0005252
CHEMBL96916 206189 0 None -19 2 Human 7.3 pKi = 7.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 365 8 1 4 3.9 C=CC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm0005252
162673916 182442 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 327 6 1 5 2.9 COc1ccc2[nH]cc(CCc3nn(CC4CCC4)c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
CHEMBL4793947 182442 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 327 6 1 5 2.9 COc1ccc2[nH]cc(CCc3nn(CC4CCC4)c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
162673578 182526 0 None -5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 272 5 2 5 2.4 CNc1nnc(CCc2c[nH]c3ccc(OC)cc23)o1 10.1016/j.ejmech.2020.112090
CHEMBL4794879 182526 0 None -5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 272 5 2 5 2.4 CNc1nnc(CCc2c[nH]c3ccc(OC)cc23)o1 10.1016/j.ejmech.2020.112090
45268318 194642 0 None -6 2 Human 5.3 pKi = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 315 4 1 4 2.2 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCCN(C)C1 10.1016/j.bmc.2009.04.068
CHEMBL562328 194642 0 None -6 2 Human 5.3 pKi = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 315 4 1 4 2.2 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCCN(C)C1 10.1016/j.bmc.2009.04.068
11109646 205333 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 309 5 2 3 3.4 CC(=O)NCCc1c(Cc2ccccc2)oc2ccc(O)cc12 10.1021/jm0005252
CHEMBL91813 205333 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 309 5 2 3 3.4 CC(=O)NCCc1c(Cc2ccccc2)oc2ccc(O)cc12 10.1021/jm0005252
122188224 122613 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 248 4 2 3 1.9 CCC(=O)NCC1CCc2c(cccc2OC)N1 10.1021/acs.jmedchem.5b01066
CHEMBL3612455 122613 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 248 4 2 3 1.9 CCC(=O)NCC1CCc2c(cccc2OC)N1 10.1021/acs.jmedchem.5b01066
53231366 62057 0 None -66 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 5 1 3 5.0 CC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
CHEMBL1779804 62057 0 None -66 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 5 1 3 5.0 CC(=O)NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12 10.1016/j.ejmech.2011.02.044
11393103 125270 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 322 5 1 3 3.8 CCC(=O)NCCN1c2ccccc2C=Cc2ccc(OC)cc21 10.1021/jm040768k
CHEMBL364806 125270 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 322 5 1 3 3.8 CCC(=O)NCCN1c2ccccc2C=Cc2ccc(OC)cc21 10.1021/jm040768k
90666304 108880 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 401 7 2 3 4.6 COc1ccc2[nH]c(Cn3ccc4ccccc43)c(CCNC(=O)C3CCC3)c2c1 10.1039/C1MD00149C
CHEMBL3219325 108880 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 401 7 2 3 4.6 COc1ccc2[nH]c(Cn3ccc4ccccc43)c(CCNC(=O)C3CCC3)c2c1 10.1039/C1MD00149C
56678563 64103 0 None 14 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 484 16 2 6 3.5 CC(=O)NCCN(C)c1cccc(OCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813320 64103 0 None 14 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 484 16 2 6 3.5 CC(=O)NCCN(C)c1cccc(OCCCCCOc2cccc(N(C)CCNC(C)=O)c2)c1 10.1016/j.bmc.2011.06.063
11529521 76391 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 298 5 2 2 3.1 COc1ccc2[nH]cc(C3(CNC(=O)C4CC4)CCC3)c2c1 10.1021/jm0512544
CHEMBL206790 76391 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 298 5 2 2 3.1 COc1ccc2[nH]cc(C3(CNC(=O)C4CC4)CCC3)c2c1 10.1021/jm0512544
122178508 120799 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 243 4 1 4 2.3 COc1ccc2[nH]cc(CCc3nnco3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580917 120799 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 243 4 1 4 2.3 COc1ccc2[nH]cc(CCc3nnco3)c2c1 10.1021/acs.jmedchem.5b00245
137633839 156057 0 None -7 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 273 5 2 3 2.1 CCNC(=O)NCCc1cccc2ncc(OC)cc12 10.1016/j.ejmech.2016.12.013
CHEMBL4068922 156057 0 None -7 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 273 5 2 3 2.1 CCNC(=O)NCCc1cccc2ncc(OC)cc12 10.1016/j.ejmech.2016.12.013
137640743 156491 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 COc1ccc2ccc(CCNC(C)=O)cc2n1 10.1016/j.ejmech.2016.12.013
CHEMBL4073867 156491 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 COc1ccc2ccc(CCNC(C)=O)cc2n1 10.1016/j.ejmech.2016.12.013
16094586 82721 4 None -213 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 311 6 1 3 3.3 COc1cccc(C(=CCNC(C)=O)c2cccc(OC)c2)c1 10.1021/jm060850a
CHEMBL218225 82721 4 None -213 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 311 6 1 3 3.3 COc1cccc(C(=CCNC(C)=O)c2cccc(OC)c2)c1 10.1021/jm060850a
145968467 164226 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 400 13 2 5 4.0 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2cccc(O)c2)c1 10.1021/acs.jmedchem.8b00893
CHEMBL4218247 164226 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 400 13 2 5 4.0 CC(=O)NCCN(C)c1cccc(OCCCCCCOc2cccc(O)c2)c1 10.1021/acs.jmedchem.8b00893
44429456 87487 0 None -8 2 Human 5.2 pKi = 5.2 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 336 6 1 3 3.9 CCC(=O)NCCc1cn(C)c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL233945 87487 0 None -8 2 Human 5.2 pKi = 5.2 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 336 6 1 3 3.9 CCC(=O)NCCc1cn(C)c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
16743288 91881 0 None -14 2 Human 5.2 pKi = 5.2 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 338 5 1 2 4.7 CCCC(=O)NCC1(c2cn3c4c(cccc24)CCC3)CCCCC1 10.1016/j.ejmech.2007.01.005
CHEMBL243003 91881 0 None -14 2 Human 5.2 pKi = 5.2 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 338 5 1 2 4.7 CCCC(=O)NCC1(c2cn3c4c(cccc24)CCC3)CCCCC1 10.1016/j.ejmech.2007.01.005
11595087 76299 0 None -6 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 328 6 1 3 3.9 CCCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCCC1 10.1021/jm0512544
CHEMBL206419 76299 0 None -6 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 328 6 1 3 3.9 CCCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CCCC1 10.1021/jm0512544
137645887 157385 0 None -58 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 294 4 1 2 3.0 CC(=O)NCC1Cc2ccccc2N(Cc2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4084568 157385 0 None -58 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 294 4 1 2 3.0 CC(=O)NCC1Cc2ccccc2N(Cc2ccccc2)C1 10.1021/acs.jmedchem.8b00359
1358 124 35 None -870 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm800974d
3976006 124 35 None -870 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm800974d
CHEMBL285718 124 35 None -870 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm800974d
44424020 84924 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 676 20 4 8 5.8 COc1ccc2[nH]c(C(=O)OCCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL226171 84924 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 676 20 4 8 5.8 COc1ccc2[nH]c(C(=O)OCCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
39847023 83967 1 None - 1 Human 4.2 pKi = 4.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 330 9 1 3 4.9 COc1cc(/C=C/C(=O)O)ccc1OC/C=C(\C)CCC=C(C)C 10.1021/acs.jnatprod.7b00853
CHEMBL221960 83967 1 None - 1 Human 4.2 pKi = 4.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 330 9 1 3 4.9 COc1cc(/C=C/C(=O)O)ccc1OC/C=C(\C)CCC=C(C)C 10.1021/acs.jnatprod.7b00853
20590665 123099 0 None 14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 391 9 1 2 5.3 CC(C)C(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL361854 123099 0 None 14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 391 9 1 2 5.3 CC(C)C(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
44358312 29593 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 3 1 3 2.0 CC(C)C(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL138744 29593 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 3 1 3 2.0 CC(C)C(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
145986330 166493 0 None -15 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 286 3 2 2 2.7 COc1ccc2ccc3c(c2c1)C(CNC(N)=S)CC3 10.1016/j.ejmech.2017.10.025
CHEMBL4289115 166493 0 None -15 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 286 3 2 2 2.7 COc1ccc2ccc3c(c2c1)C(CNC(N)=S)CC3 10.1016/j.ejmech.2017.10.025
18522272 65743 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 375 10 1 2 5.5 O=C(NCCCc1cccc2oc(CCCCc3ccccc3)cc12)C1CC1 10.1016/j.bmcl.2004.07.055
CHEMBL183846 65743 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 375 10 1 2 5.5 O=C(NCCCc1cccc2oc(CCCCc3ccccc3)cc12)C1CC1 10.1016/j.bmcl.2004.07.055
145972981 163932 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 513 13 3 4 6.2 CC(=O)NCCc1c[nH]c2ccc(OCCCCCCNC(=O)Oc3cccc(-c4ccccc4)c3)cc12 10.1021/acs.jmedchem.8b00893
CHEMBL4214478 163932 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 513 13 3 4 6.2 CC(=O)NCCc1c[nH]c2ccc(OCCCCCCNC(=O)Oc3cccc(-c4ccccc4)c3)cc12 10.1021/acs.jmedchem.8b00893
11507534 165569 0 None -5 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 288 5 1 3 3.0 CCC(=O)NCC(C)(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
CHEMBL426127 165569 0 None -5 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 288 5 1 3 3.0 CCC(=O)NCC(C)(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
11185529 3839 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm040768k
7772 3839 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm040768k
CHEMBL189449 3839 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm040768k
127041168 136068 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 388 10 2 3 3.9 O=C(NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12)C(F)F 10.1039/C5MD00190K
CHEMBL3739674 136068 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 388 10 2 3 3.9 O=C(NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12)C(F)F 10.1039/C5MD00190K
11185529 3839 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm048956y
7772 3839 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm048956y
CHEMBL189449 3839 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm048956y
127041168 136068 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 388 10 2 3 3.9 O=C(NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12)C(F)F 10.1039/C5MD00190K
CHEMBL3739674 136068 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 388 10 2 3 3.9 O=C(NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12)C(F)F 10.1039/C5MD00190K
10611901 23358 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 267 5 1 1 3.8 CCCC(=O)NCCC1Cc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL133426 23358 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 267 5 1 1 3.8 CCCC(=O)NCCC1Cc2cccc3cccc1c23 10.1021/jm000922c
10801655 21160 0 None 2 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 265 4 1 1 3.4 O=C(NCCC1Cc2cccc3cccc1c23)C1CC1 10.1021/jm000922c
CHEMBL131431 21160 0 None 2 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 265 4 1 1 3.4 O=C(NCCC1Cc2cccc3cccc1c23)C1CC1 10.1021/jm000922c
10800029 116197 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 239 3 1 1 3.0 CC(=O)NCCC1Cc2cccc3cccc1c23 10.1021/jm000922c
CHEMBL337295 116197 0 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 239 3 1 1 3.0 CC(=O)NCCC1Cc2cccc3cccc1c23 10.1021/jm000922c
44358275 167877 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 287 3 2 3 1.7 O=C(NC1CC1)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL435023 167877 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 287 3 2 3 1.7 O=C(NC1CC1)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
22718564 16586 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 5 1 3 2.3 CCC(=O)NCCCc1cccc2ncoc12 10.1016/j.bmcl.2004.04.082
CHEMBL124476 16586 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 232 5 1 3 2.3 CCC(=O)NCCCc1cccc2ncoc12 10.1016/j.bmcl.2004.04.082
44241665 194017 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 329 6 1 4 2.6 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCN(C)C2 10.1016/j.bmc.2009.04.068
CHEMBL556908 194017 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 329 6 1 4 2.6 CCCC(=O)NCCc1c2n(c3ccc(OC)cc13)CCN(C)C2 10.1016/j.bmc.2009.04.068
44426096 85295 0 None -4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 211 2 1 1 2.9 CC(=O)N/C=C/c1cccc2ccccc12 10.1016/j.bmcl.2012.11.069
CHEMBL229015 85295 0 None -4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 211 2 1 1 2.9 CC(=O)N/C=C/c1cccc2ccccc12 10.1016/j.bmcl.2012.11.069
10061064 102482 0 None -7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 258 5 1 3 2.3 CCC(=O)NCCc1ccnc2ccc(OC)cc12 10.1016/S0960-894X(97)00392-2
CHEMBL306468 102482 0 None -7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cellsBinding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells
ChEMBL 258 5 1 3 2.3 CCC(=O)NCCc1ccnc2ccc(OC)cc12 10.1016/S0960-894X(97)00392-2
44389768 64197 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 426 9 2 2 5.5 CCNC(=O)NC[C@@H]1C[C@H]1c1c(Cl)ccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL181457 64197 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 426 9 2 2 5.5 CCNC(=O)NC[C@@H]1C[C@H]1c1c(Cl)ccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
22718654 112820 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 7 1 3 3.5 CCCc1nc2cccc(CCCNC(=O)C(C)C)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL331636 112820 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 288 7 1 3 3.5 CCCc1nc2cccc(CCCNC(=O)C(C)C)c2o1 10.1016/j.bmcl.2004.04.082
22718596 116857 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 322 7 1 3 4.3 CCCC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL339784 116857 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 322 7 1 3 4.3 CCCC(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
137655435 158252 0 None -15 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 COc1cnc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2016.12.013
CHEMBL4094436 158252 0 None -15 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 COc1cnc2cccc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2016.12.013
12985495 180794 0 None -213 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 377 8 2 3 4.5 CCCC(=O)NCCc1cc(-c2cccc(CO)c2)cc2ccc(OC)cc12 10.1016/j.bmc.2008.08.052
CHEMBL476341 180794 0 None -213 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 377 8 2 3 4.5 CCCC(=O)NCCc1cc(-c2cccc(CO)c2)cc2ccc(OC)cc12 10.1016/j.bmc.2008.08.052
122162 2345 67 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm980684+
1363 2345 67 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm980684+
CHEMBL286615 2345 67 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm980684+
44264706 202715 1 None -33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 270 5 2 3 3.8 CCC(=O)Nc1ccc(Nc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7215 202715 1 None -33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 270 5 2 3 3.8 CCC(=O)Nc1ccc(Nc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
44264689 203332 1 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 282 5 2 3 3.8 COc1cccc(Nc2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL7713 203332 1 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 282 5 2 3 3.8 COc1cccc(Nc2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
90666308 108884 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 389 7 2 3 3.8 COc1ccc2[nH]c(CN3Cc4ccccc4C3)c(CCNC(=O)C3CC3)c2c1 10.1039/C1MD00149C
CHEMBL3219329 108884 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 389 7 2 3 3.8 COc1ccc2[nH]c(CN3Cc4ccccc4C3)c(CCNC(=O)C3CC3)c2c1 10.1039/C1MD00149C
44429453 87099 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 322 6 2 2 3.9 CCC(=O)NCCc1c[nH]c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL233517 87099 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 322 6 2 2 3.9 CCC(=O)NCCc1c[nH]c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
3964826 15663 30 None -1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1ccc(OCCNC(C)=O)cc1 10.1016/j.bmc.2010.06.100
CHEMBL1223054 15663 30 None -1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1ccc(OCCNC(C)=O)cc1 10.1016/j.bmc.2010.06.100
44412063 77220 0 None 2 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 298 4 2 3 2.8 Cn1cc(C2(CNC(=O)C3CC3)CCC2)c2cc(O)ccc21 10.1021/jm0512544
CHEMBL208802 77220 0 None 2 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 298 4 2 3 2.8 Cn1cc(C2(CNC(=O)C3CC3)CCC2)c2cc(O)ccc21 10.1021/jm0512544
137637541 155445 0 None -269 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 293 4 1 1 3.9 CCC(=O)NC[C@@H]1CCc2ccccc2[C@H]1c1ccccc1 10.1021/acs.jmedchem.8b00359
CHEMBL4061850 155445 0 None -269 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 293 4 1 1 3.9 CCC(=O)NC[C@@H]1CCc2ccccc2[C@H]1c1ccccc1 10.1021/acs.jmedchem.8b00359
9947753 203182 0 None -83 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 285 6 1 3 4.2 CCCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7599 203182 0 None -83 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 285 6 1 3 4.2 CCCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
44264949 203250 0 None -83 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 299 7 1 3 4.6 CCCCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7650 203250 0 None -83 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 299 7 1 3 4.6 CCCCC(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
145990308 166468 0 None -20 3 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 328 5 2 2 3.8 CCCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4288690 166468 0 None -20 3 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 328 5 2 2 3.8 CCCNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
10567865 4099 0 None -38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 322 6 1 3 3.7 CCC(=O)NCCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm001125h
CHEMBL100104 4099 0 None -38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 322 6 1 3 3.7 CCC(=O)NCCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm001125h
10567865 4099 0 None -38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 322 6 1 3 3.7 CCC(=O)NCCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm970721h
CHEMBL100104 4099 0 None -38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 322 6 1 3 3.7 CCC(=O)NCCc1cc2c(OC)cccc2n1-c1ccccc1 10.1021/jm970721h
10639585 113952 0 None -83 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 322 6 1 3 3.7 CCC(=O)NCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm001125h
CHEMBL33346 113952 0 None -83 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 322 6 1 3 3.7 CCC(=O)NCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm001125h
10513751 162731 1 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1cccc2[nH]c(CCNC(C)=O)cc12 10.1021/jm001125h
CHEMBL418789 162731 1 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1cccc2[nH]c(CCNC(C)=O)cc12 10.1021/jm001125h
10639585 113952 0 None -83 2 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 322 6 1 3 3.7 CCC(=O)NCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm970721h
CHEMBL33346 113952 0 None -83 2 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 322 6 1 3 3.7 CCC(=O)NCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm970721h
10513751 162731 1 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1cccc2[nH]c(CCNC(C)=O)cc12 10.1021/jm970721h
CHEMBL418789 162731 1 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1cccc2[nH]c(CCNC(C)=O)cc12 10.1021/jm970721h
11310062 15737 2 None -1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)N[C@H](C)COc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223274 15737 2 None -1 2 Human 4.2 pKi = 4.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 193 4 1 2 1.6 CC(=O)N[C@H](C)COc1ccccc1 10.1016/j.bmc.2010.06.100
122188345 122632 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 334 5 1 2 3.9 O=C(NCC1CCc2ccccc2N1Cc1ccccc1)C1CCC1 10.1021/acs.jmedchem.5b01066
CHEMBL3612602 122632 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 334 5 1 2 3.9 O=C(NCC1CCc2ccccc2N1Cc1ccccc1)C1CCC1 10.1021/acs.jmedchem.5b01066
10969292 206087 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 321 6 1 2 4.3 CCc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL96333 206087 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 321 6 1 2 4.3 CCc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
44424025 84736 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 504 14 4 4 4.6 COc1ccc2[nH]cc(CCNC(=O)CCCCCC(=O)NCCc3c[nH]c4ccc(OC)cc34)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL225302 84736 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 504 14 4 4 4.6 COc1ccc2[nH]cc(CCNC(=O)CCCCCC(=O)NCCc3c[nH]c4ccc(OC)cc34)c2c1 10.1016/j.bmc.2007.03.080
11680808 76711 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 5 2 2 3.1 CCC(=O)NCC1(c2c[nH]c3ccc(OC)cc23)CCC1 10.1021/jm0512544
CHEMBL207420 76711 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 5 2 2 3.1 CCC(=O)NCC1(c2c[nH]c3ccc(OC)cc23)CCC1 10.1021/jm0512544
1359 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm800974d
5311198 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm800974d
CHEMBL274438 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm800974d
1359 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm048956y
5311198 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm048956y
CHEMBL274438 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm048956y
1359 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm980684+
5311198 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm980684+
CHEMBL274438 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm980684+
1359 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm401343c
5311198 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm401343c
CHEMBL274438 2130 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm401343c
10925526 111829 0 None -26 2 Human 7.2 pKi = 7.2 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 329 6 1 3 4.2 COc1ccc2oc(CC3CCCCC3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL329299 111829 0 None -26 2 Human 7.2 pKi = 7.2 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 329 6 1 3 4.2 COc1ccc2oc(CC3CCCCC3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
44357899 118163 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 4 1 3 2.1 CCCC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL341705 118163 0 None -3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 274 4 1 3 2.1 CCCC(=O)N[C@@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
118712372 113640 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 308 2 1 2 3.4 CCNC(=O)N1CCCC2Cc3cc(Cl)c(OC)cc3C21 10.1016/j.ejmech.2014.09.038
CHEMBL3329390 113640 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting
ChEMBL 308 2 1 2 3.4 CCNC(=O)N1CCCC2Cc3cc(Cl)c(OC)cc3C21 10.1016/j.ejmech.2014.09.038
127040355 137374 0 None -13 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 410 5 1 4 5.5 COc1ccc2oc(-c3cc4ccccc4c4ccccc34)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
CHEMBL3763537 137374 0 None -13 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 410 5 1 4 5.5 COc1ccc2oc(-c3cc4ccccc4c4ccccc34)c(CCNC(C)=O)c2n1 10.1016/j.ejmech.2016.01.008
16094580 81132 4 None -11 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 283 6 1 2 3.0 COc1ccc(Cc2ccccc2)c(CCNC(C)=O)c1 10.1021/jm060850a
CHEMBL216158 81132 4 None -11 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 283 6 1 2 3.0 COc1ccc(Cc2ccccc2)c(CCNC(C)=O)c1 10.1021/jm060850a
137657824 159238 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 289 5 2 3 2.3 CCNC(=S)NCCc1cccc2ncc(OC)cc12 10.1016/j.ejmech.2016.12.013
CHEMBL4105511 159238 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 289 5 2 3 2.3 CCNC(=S)NCCc1cccc2ncc(OC)cc12 10.1016/j.ejmech.2016.12.013
162668486 181982 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 377 8 1 5 3.7 COc1ccc2[nH]cc(CCc3nn(CCCc4ccccc4)c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
CHEMBL4787877 181982 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysisDisplacement of [125l]-lodomelatonin from human MT1 receptor expressed in CHO cells incubated for 120 mins by scintillation counting analysis
ChEMBL 377 8 1 5 3.7 COc1ccc2[nH]cc(CCc3nn(CCCc4ccccc4)c(=O)o3)c2c1 10.1016/j.ejmech.2020.112090
10893437 206697 0 None -6 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 348 6 1 3 4.1 COc1cccc2c1cc(CCNC(=O)C1CCC1)n2-c1ccccc1 10.1021/jm001125h
CHEMBL99987 206697 0 None -6 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 348 6 1 3 4.1 COc1cccc2c1cc(CCNC(=O)C1CCC1)n2-c1ccccc1 10.1021/jm001125h
16094591 82896 4 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 283 6 1 2 3.2 COc1cccc(C(CNC(C)=O)Cc2ccccc2)c1 10.1021/jm060850a
CHEMBL219127 82896 4 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 283 6 1 2 3.2 COc1cccc(C(CNC(C)=O)Cc2ccccc2)c1 10.1021/jm060850a
10948786 206055 0 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 375 7 1 4 4.6 COc1ccc2oc(Cc3ccccc3)c(CCNC(=O)c3ccco3)c2c1 10.1021/jm0005252
CHEMBL96173 206055 0 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 375 7 1 4 4.6 COc1ccc2oc(Cc3ccccc3)c(CCNC(=O)c3ccco3)c2c1 10.1021/jm0005252
44358231 26727 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 275 3 2 3 1.5 CCNC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
CHEMBL136431 26727 0 None -3 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 275 3 2 3 1.5 CCNC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
145979585 165926 0 None -17 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 313 5 2 3 3.0 CCCNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4278446 165926 0 None -17 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 313 5 2 3 3.0 CCCNC(=O)NCC1CCc2ccc3ccc(OC)nc3c21 10.1016/j.ejmech.2017.10.025
145991111 166348 0 None -17 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 319 5 1 3 2.8 CCS(=O)(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4286494 166348 0 None -17 3 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 319 5 1 3 2.8 CCS(=O)(=O)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
137645530 157169 0 None -23 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 260 4 1 4 2.1 COC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4082097 157169 0 None -23 2 Human 8.2 pKi = 8.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 260 4 1 4 2.1 COC(=O)NCCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
11002840 205784 0 None -33 2 Human 8.1 pKi = 8.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 357 6 1 3 4.4 COc1ccc2oc(Cc3cccc(Cl)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL94607 205784 0 None -33 2 Human 8.1 pKi = 8.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 357 6 1 3 4.4 COc1ccc2oc(Cc3cccc(Cl)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
10616723 97840 0 None -14 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 334 4 1 3 3.6 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCc2ccccc2-1 10.1021/jm980684+
CHEMBL274842 97840 0 None -14 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 334 4 1 3 3.6 COc1ccc2c(c1)c(CCNC(C)=O)c1n2CCc2ccccc2-1 10.1021/jm980684+
44436051 150819 6 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 209 5 1 3 1.2 COc1cccc(OCCNC(C)=O)c1 10.1021/jm700957j
CHEMBL396132 150819 6 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 209 5 1 3 1.2 COc1cccc(OCCNC(C)=O)c1 10.1021/jm700957j
10384120 123859 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 363 10 1 2 5.5 CCC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
CHEMBL363936 123859 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1AInhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A
ChEMBL 363 10 1 2 5.5 CCC(=O)NCCCc1cccc2oc(CCCCc3ccccc3)cc12 10.1016/j.bmcl.2004.07.055
44317725 203948 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 329 9 1 3 4.1 CCCCOc1ccc2ccc(OC)cc2c1CCNC(=O)CC 10.1016/S0960-894X(97)00444-7
CHEMBL82135 203948 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 329 9 1 3 4.1 CCCCOc1ccc2ccc(OC)cc2c1CCNC(=O)CC 10.1016/S0960-894X(97)00444-7
11644612 77880 0 None -9 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.4 COc1ccc2c(c1)c(C(C)CNC(C)=O)cn2C 10.1021/jm0512544
CHEMBL210791 77880 0 None -9 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.4 COc1ccc2c(c1)c(C(C)CNC(C)=O)cn2C 10.1021/jm0512544
168288029 191015 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 471 9 1 9 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
CHEMBL5195595 191015 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assayDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes in presence of light-activated compounds by radioligand based competition binding assay
ChEMBL 471 9 1 9 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1cc(OC)c(OC)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
49865269 15687 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 249 6 1 3 2.0 COc1cccc(O[C@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223129 15687 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 249 6 1 3 2.0 COc1cccc(O[C@H](C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
56653479 110368 0 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 352 9 2 3 3.7 CC(=O)NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3260986 110368 0 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 352 9 2 3 3.7 CC(=O)NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
56653479 110368 0 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 352 9 2 3 3.7 CC(=O)NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12 10.1021/jm401343c
CHEMBL3260986 110368 0 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 352 9 2 3 3.7 CC(=O)NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12 10.1021/jm401343c
16750566 141488 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 662 19 4 8 5.4 COc1ccc2[nH]c(C(=O)OCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL387655 141488 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 662 19 4 8 5.4 COc1ccc2[nH]c(C(=O)OCCCCCCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
56653479 110368 0 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 352 9 2 3 3.7 CC(=O)NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3260986 110368 0 None 10 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 352 9 2 3 3.7 CC(=O)NCCc1c[nH]c2ccc(OCCCOc3ccccc3)cc12 10.1039/C5MD00190K
44424023 144269 0 None -14 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 346 9 2 4 3.2 CCCCCOC(=O)c1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1016/j.bmc.2007.03.080
CHEMBL390944 144269 0 None -14 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 346 9 2 4 3.2 CCCCCOC(=O)c1[nH]c2ccc(OC)cc2c1CCNC(C)=O 10.1016/j.bmc.2007.03.080
49865323 15709 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 267 7 1 3 3.1 CCCC(=O)NC[C@@H](C)Sc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223197 15709 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 267 7 1 3 3.1 CCCC(=O)NC[C@@H](C)Sc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
10711649 206039 0 None -19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 332 5 1 2 4.3 CCCC(=O)NCCc1c2n(c3ccccc13)CCc1ccccc1-2 10.1021/jm980684+
CHEMBL9605 206039 0 None -19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 332 5 1 2 4.3 CCCC(=O)NCCc1c2n(c3ccccc13)CCc1ccccc1-2 10.1021/jm980684+
16094576 137591 6 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 253 5 1 1 3.1 CC(=O)NCC(Cc1ccccc1)c1ccccc1 10.1021/jm060850a
CHEMBL376693 137591 6 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 253 5 1 1 3.1 CC(=O)NCC(Cc1ccccc1)c1ccccc1 10.1021/jm060850a
81689735 120798 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 257 4 1 4 2.7 COc1ccc2[nH]cc(CCc3nnc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3580916 120798 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 257 4 1 4 2.7 COc1ccc2[nH]cc(CCc3nnc(C)o3)c2c1 10.1021/acs.jmedchem.5b00245
CHEMBL3109560 209332 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 minsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 mins
ChEMBL None None None COc1ccc(/C=C/C2=[N+]3C(=Cc4c(CCNC(C)=O)c5cc(OC)ccc5n4[B-]3(F)F)C=C2)cc1 10.1021/ml4004155
681 1432 65 None -38 39 Human 5.2 pKi = 5.2 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(97)00444-7
940 1432 65 None -38 39 Human 5.2 pKi = 5.2 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(97)00444-7
947 1432 65 None -38 39 Human 5.2 pKi = 5.2 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(97)00444-7
CHEMBL59 1432 65 None -38 39 Human 5.2 pKi = 5.2 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(97)00444-7
DB00988 1432 65 None -38 39 Human 5.2 pKi = 5.2 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(97)00444-7
11624018 140344 0 None 5 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 326 5 1 3 3.5 COc1ccc2c(c1)c(C1(CNC(=O)C3CCC3)CCC1)cn2C 10.1021/jm0512544
CHEMBL382050 140344 0 None 5 2 Human 6.2 pKi = 6.2 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 326 5 1 3 3.5 COc1ccc2c(c1)c(C1(CNC(=O)C3CCC3)CCC1)cn2C 10.1021/jm0512544
44412082 138736 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 5 2 3 3.2 CCCC(=O)NCC1(c2cn(C)c3ccc(O)cc23)CCC1 10.1021/jm0512544
CHEMBL379096 138736 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 300 5 2 3 3.2 CCCC(=O)NCC1(c2cn(C)c3ccc(O)cc23)CCC1 10.1021/jm0512544
127025781 137286 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 309 5 1 3 3.7 COc1ccc2ccc3oc(CCNC(=O)C4CC4)cc3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759859 137286 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 309 5 1 3 3.7 COc1ccc2ccc3oc(CCNC(=O)C4CC4)cc3c2c1 10.1016/j.ejmech.2015.12.047
127039218 137357 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 234 4 1 4 1.5 COc1cc2c(CCNC(C)=O)coc2cn1 10.1016/j.ejmech.2016.01.008
CHEMBL3763247 137357 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 234 4 1 4 1.5 COc1cc2c(CCNC(C)=O)coc2cn1 10.1016/j.ejmech.2016.01.008
56671858 64108 0 None -20 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 498 17 2 6 3.8 COc1cccc(N(CCCCCCN(CCNC(C)=O)c2cccc(OC)c2)CCNC(C)=O)c1 10.1016/j.bmc.2011.06.063
CHEMBL1813325 64108 0 None -20 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membraneDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in mouse NIH-3T3 cell membrane
ChEMBL 498 17 2 6 3.8 COc1cccc(N(CCCCCCN(CCNC(C)=O)c2cccc(OC)c2)CCNC(C)=O)c1 10.1016/j.bmc.2011.06.063
49865424 15768 0 None -1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 4 1 2 2.3 CC(=O)N[C@H](C)CSc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223346 15768 0 None -1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 4 1 2 2.3 CC(=O)N[C@H](C)CSc1ccccc1 10.1016/j.bmc.2010.06.100
44349171 16461 1 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 275 6 2 3 2.6 CCNC(=O)NCCCc1cccc2nc(CC)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL124217 16461 1 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 275 6 2 3 2.6 CCNC(=O)NCCCc1cccc2nc(CC)oc12 10.1016/j.bmcl.2004.04.082
16743123 92630 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 270 5 1 2 3.0 CCC(=O)NCCCc1cn2c3c(cccc13)CCC2 10.1016/j.ejmech.2007.01.005
CHEMBL244263 92630 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 270 5 1 2 3.0 CCC(=O)NCCCc1cn2c3c(cccc13)CCC2 10.1016/j.ejmech.2007.01.005
11794657 206570 0 None -23 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 388 5 1 3 4.7 COc1ccc2c(c1)c(CCNC(=O)C1CCC1)c1n2CCCc2ccccc2-1 10.1021/jm980684+
CHEMBL9917 206570 0 None -23 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 388 5 1 3 4.7 COc1ccc2c(c1)c(CCNC(=O)C1CCC1)c1n2CCCc2ccccc2-1 10.1021/jm980684+
10567427 4160 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 316 4 1 2 3.7 O=C(NCCc1c2n(c3ccccc13)Cc1ccccc1-2)C1CC1 10.1021/jm980684+
CHEMBL10043 4160 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 316 4 1 2 3.7 O=C(NCCc1c2n(c3ccccc13)Cc1ccccc1-2)C1CC1 10.1021/jm980684+
24749950 3841 6 None -588 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1ccc(cc1)N(c1ccccc1)CCNC(=O)C 10.1021/jm700957j
7923 3841 6 None -588 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1ccc(cc1)N(c1ccccc1)CCNC(=O)C 10.1021/jm700957j
CHEMBL394676 3841 6 None -588 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1ccc(cc1)N(c1ccccc1)CCNC(=O)C 10.1021/jm700957j
9859693 73762 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 246 6 0 3 3.3 COc1cc(/C=C/C=O)ccc1OCC=C(C)C 10.1021/acs.jnatprod.7b00853
CHEMBL2022666 73762 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 246 6 0 3 3.3 COc1cc(/C=C/C=O)ccc1OCC=C(C)C 10.1021/acs.jnatprod.7b00853
10807560 206396 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 346 5 1 2 4.7 CCCC(=O)NCCc1c2n(c3ccccc13)CCCc1ccccc1-2 10.1021/jm980684+
CHEMBL9815 206396 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 346 5 1 2 4.7 CCCC(=O)NCCc1c2n(c3ccccc13)CCCc1ccccc1-2 10.1021/jm980684+
122162 2345 67 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1016/j.ejmech.2007.01.005
1363 2345 67 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1016/j.ejmech.2007.01.005
CHEMBL286615 2345 67 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1016/j.ejmech.2007.01.005
10044270 188943 0 None -891 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 1 2 4.8 COc1ccc2c(c1)[C@@H](CCNC(=O)C1CCC1)C[C@@H](c1ccccc1)C2 10.1021/jm800974d
CHEMBL514280 188943 0 None -891 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 1 2 4.8 COc1ccc2c(c1)[C@@H](CCNC(=O)C1CCC1)C[C@@H](c1ccccc1)C2 10.1021/jm800974d
45270052 193712 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 381 8 2 4 3.5 COc1ccc(N(C)Cc2[nH]c3ccc(OC)cc3c2CCNC(C)=O)cc1 10.1016/j.bmc.2009.04.068
CHEMBL552002 193712 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 381 8 2 4 3.5 COc1ccc(N(C)Cc2[nH]c3ccc(OC)cc3c2CCNC(C)=O)cc1 10.1016/j.bmc.2009.04.068
137650611 156958 0 None -26 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 CNC(=O)CCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
CHEMBL4079784 156958 0 None -26 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 244 4 1 3 1.9 CNC(=O)CCc1cccc2ccc(OC)nc12 10.1016/j.ejmech.2016.12.013
9970584 16577 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 7 1 3 3.2 CCCC(=O)NCCCc1cccc2nc(CC)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL124422 16577 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 274 7 1 3 3.2 CCCC(=O)NCCCc1cccc2nc(CC)oc12 10.1016/j.bmcl.2004.04.082
44317822 104384 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 315 8 1 3 3.7 CCCOc1ccc2ccc(OC)cc2c1CCNC(=O)CC 10.1016/S0960-894X(97)00444-7
CHEMBL311106 104384 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 315 8 1 3 3.7 CCCOc1ccc2ccc(OC)cc2c1CCNC(=O)CC 10.1016/S0960-894X(97)00444-7
45270052 193712 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 381 8 2 4 3.5 COc1ccc(N(C)Cc2[nH]c3ccc(OC)cc3c2CCNC(C)=O)cc1 10.1016/j.bmc.2009.04.068
CHEMBL552002 193712 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma countingDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting
ChEMBL 381 8 2 4 3.5 COc1ccc(N(C)Cc2[nH]c3ccc(OC)cc3c2CCNC(C)=O)cc1 10.1016/j.bmc.2009.04.068
10938056 106562 0 None -2 2 Human 8.1 pKi = 8.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 393 11 1 3 5.7 CCCCCCOc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL315653 106562 0 None -2 2 Human 8.1 pKi = 8.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 393 11 1 3 5.7 CCCCCCOc1ccc2oc(Cc3ccccc3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
11637615 76879 0 None -2 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 272 4 2 2 2.7 COc1ccc2[nH]cc(C3(CNC(C)=O)CCC3)c2c1 10.1021/jm0512544
CHEMBL207960 76879 0 None -2 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 272 4 2 2 2.7 COc1ccc2[nH]cc(C3(CNC(C)=O)CCC3)c2c1 10.1021/jm0512544
11681026 76772 0 None -11 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 302 6 1 3 3.4 CCCC(=O)NCC(C)(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
CHEMBL207745 76772 0 None -11 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 302 6 1 3 3.4 CCCC(=O)NCC(C)(C)c1cn(C)c2ccc(OC)cc12 10.1021/jm0512544
49865270 15689 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 265 6 1 3 2.7 COc1cccc(SC(C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223131 15689 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 265 6 1 3 2.7 COc1cccc(SC(C)CNC(=O)C2CC2)c1 10.1016/j.bmc.2010.06.100
11733059 111150 0 None -21 2 Human 8.1 pKi = 8.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 449 7 1 3 4.1 COc1ccc2oc(Cc3ccccc3)c(CCNC(=O)CI)c2c1 10.1021/jm0005252
CHEMBL328617 111150 0 None -21 2 Human 8.1 pKi = 8.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 449 7 1 3 4.1 COc1ccc2oc(Cc3ccccc3)c(CCNC(=O)CI)c2c1 10.1021/jm0005252
44429444 146186 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.2 COc1cc(C)c2c(c1)c(CCNC(C)=O)cn2C 10.1016/j.bmc.2007.04.013
CHEMBL392421 146186 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 1 3 2.2 COc1cc(C)c2c(c1)c(CCNC(C)=O)cn2C 10.1016/j.bmc.2007.04.013
9860588 19731 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 4 1 2 3.4 COc1ccc2cccc3c2c1CCC3CCNC(C)=O 10.1021/jm000922c
CHEMBL130286 19731 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 4 1 2 3.4 COc1ccc2cccc3c2c1CCC3CCNC(C)=O 10.1021/jm000922c
10522674 206016 0 None -56 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 7 1 3 4.5 CCCC(=O)NCCc1c2n(c3ccc(OCC)cc13)Cc1ccccc1-2 10.1021/jm980684+
CHEMBL9590 206016 0 None -56 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 362 7 1 3 4.5 CCCC(=O)NCCc1c2n(c3ccc(OCC)cc13)Cc1ccccc1-2 10.1021/jm980684+
11784134 106453 0 None -67 2 Human 7.1 pKi = 7.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 391 6 1 3 4.7 COc1ccc2oc(Cc3cccc(C(F)(F)F)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL314947 106453 0 None -67 2 Human 7.1 pKi = 7.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 391 6 1 3 4.7 COc1ccc2oc(Cc3cccc(C(F)(F)F)c3)c(CCNC(C)=O)c2c1 10.1021/jm0005252
49865320 15706 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 251 7 1 3 2.4 CCCC(=O)NC[C@@H](C)Oc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223194 15706 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 251 7 1 3 2.4 CCCC(=O)NC[C@@H](C)Oc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
1354 3369 10 None -275 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 10.1016/j.bmc.2008.08.052
22133318 3369 10 None -275 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 10.1016/j.bmc.2008.08.052
CHEMBL490188 3369 10 None -275 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 10.1016/j.bmc.2008.08.052
44579115 181243 0 None -162 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 348 6 2 3 4.2 CNc1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
CHEMBL477835 181243 0 None -162 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 348 6 2 3 4.2 CNc1cccc(-c2cc(CCNC(C)=O)c3cc(OC)ccc3c2)c1 10.1016/j.bmc.2008.08.052
54583162 60422 0 None -7 2 Human 5.1 pKi = 5.1 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 276 6 2 5 0.9 CNCc1cn(CCNC(C)=O)c2nc(OC)ccc12 10.1016/j.bmcl.2011.02.097
CHEMBL1760954 60422 0 None -7 2 Human 5.1 pKi = 5.1 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 276 6 2 5 0.9 CNCc1cn(CCNC(C)=O)c2nc(OC)ccc12 10.1016/j.bmcl.2011.02.097
137653199 158065 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 218 2 1 2 1.4 CC(=O)NCC1Cc2ccccc2N(C)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4092308 158065 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 218 2 1 2 1.4 CC(=O)NCC1Cc2ccccc2N(C)C1 10.1021/acs.jmedchem.8b00359
44424024 84735 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 522 16 2 6 5.6 COc1ccc2[nH]c(C(=O)OCCCCCCCCCOC(=O)c3ccccc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL225301 84735 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 522 16 2 6 5.6 COc1ccc2[nH]c(C(=O)OCCCCCCCCCOC(=O)c3ccccc3)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
10640625 206545 0 None -46 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 336 7 1 3 3.8 CCC(=O)NCCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm001125h
CHEMBL99002 206545 0 None -46 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 336 7 1 3 3.8 CCC(=O)NCCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm001125h
10640625 206545 0 None -46 2 Human 6.1 pKi = 6.1 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 336 7 1 3 3.8 CCC(=O)NCCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm970721h
CHEMBL99002 206545 0 None -46 2 Human 6.1 pKi = 6.1 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 336 7 1 3 3.8 CCC(=O)NCCc1cc2c(OC)cccc2n1Cc1ccccc1 10.1021/jm970721h
44264707 96710 1 None -19 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 256 4 2 3 3.4 COc1cccc(Nc2ccc(NC(C)=O)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL268165 96710 1 None -19 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 256 4 2 3 3.4 COc1cccc(Nc2ccc(NC(C)=O)cc2)c1 10.1016/j.bmcl.2003.11.030
9859913 203809 0 None -20 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 257 4 1 3 3.4 COc1cccc(Oc2ccc(NC(C)=O)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL8094 203809 0 None -20 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 257 4 1 3 3.4 COc1cccc(Oc2ccc(NC(C)=O)cc2)c1 10.1016/j.bmcl.2003.11.030
9930390 206134 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 391 6 1 3 5.0 COc1ccc2oc(Cc3c(Cl)cccc3Cl)c(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL96562 206134 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 391 6 1 3 5.0 COc1ccc2oc(Cc3c(Cl)cccc3Cl)c(CCNC(C)=O)c2c1 10.1021/jm0005252
25209999 174935 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 441 6 2 3 4.2 COc1ccc2[nH]c(CN3CCc4cc(Br)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL457807 174935 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 441 6 2 3 4.2 COc1ccc2[nH]c(CN3CCc4cc(Br)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
25209999 174935 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 441 6 2 3 4.2 COc1ccc2[nH]c(CN3CCc4cc(Br)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
CHEMBL457807 174935 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 441 6 2 3 4.2 COc1ccc2[nH]c(CN3CCc4cc(Br)ccc43)c(CCNC(C)=O)c2c1 10.1021/jm800974d
10104923 101017 2 None -12 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 221 6 1 2 2.2 CCC(=O)NCCCc1cccc(OC)c1 10.1016/j.bmcl.2010.02.084
CHEMBL297947 101017 2 None -12 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 221 6 1 2 2.2 CCC(=O)NCCCc1cccc(OC)c1 10.1016/j.bmcl.2010.02.084
10609620 206558 1 None -5 2 Human 5.1 pKi = 5.1 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2cc(CCNC(C)=O)[nH]c2c1 10.1021/jm001125h
CHEMBL99091 206558 1 None -5 2 Human 5.1 pKi = 5.1 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 232 4 2 2 1.9 COc1ccc2cc(CCNC(C)=O)[nH]c2c1 10.1021/jm001125h
10609620 206558 1 None -5 2 Human 5.1 pKi = 5.1 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2cc(CCNC(C)=O)[nH]c2c1 10.1021/jm970721h
CHEMBL99091 206558 1 None -5 2 Human 5.1 pKi = 5.1 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2cc(CCNC(C)=O)[nH]c2c1 10.1021/jm970721h
10946222 193063 0 None -43 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 291 5 1 5 1.8 COc1ccc2c(c(CCNC(C)=O)cn2C)c1[N+](=O)[O-] 10.1021/jm011053+
CHEMBL53622 193063 0 None -43 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 291 5 1 5 1.8 COc1ccc2c(c(CCNC(C)=O)cn2C)c1[N+](=O)[O-] 10.1021/jm011053+
11623375 138150 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 5 1 3 2.7 CCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CC1 10.1021/jm0512544
CHEMBL377871 138150 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 286 5 1 3 2.7 CCC(=O)NCC1(c2cn(C)c3ccc(OC)cc23)CC1 10.1021/jm0512544
22718548 16309 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 322 6 1 3 4.2 CC(C)C(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
CHEMBL123612 16309 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 322 6 1 3 4.2 CC(C)C(=O)NCCCc1cccc2nc(-c3ccccc3)oc12 10.1016/j.bmcl.2004.04.082
71540390 85977 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 235 4 1 3 1.7 COc1ccc(OC)c([C@@H]2C[C@H]2NC(C)=O)c1 10.1016/j.bmcl.2012.11.069
CHEMBL2314263 85977 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 235 4 1 3 1.7 COc1ccc(OC)c([C@@H]2C[C@H]2NC(C)=O)c1 10.1016/j.bmcl.2012.11.069
10518884 112049 0 None -11 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 308 5 1 3 3.3 COc1cccc2c1cc(CCNC(C)=O)n2-c1ccccc1 10.1021/jm001125h
CHEMBL329979 112049 0 None -11 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 308 5 1 3 3.3 COc1cccc2c1cc(CCNC(C)=O)n2-c1ccccc1 10.1021/jm001125h
10518884 112049 0 None -11 2 Human 7.1 pKi = 7.1 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 308 5 1 3 3.3 COc1cccc2c1cc(CCNC(C)=O)n2-c1ccccc1 10.1021/jm970721h
CHEMBL329979 112049 0 None -11 2 Human 7.1 pKi = 7.1 Binding
Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cellsBinding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells
ChEMBL 308 5 1 3 3.3 COc1cccc2c1cc(CCNC(C)=O)n2-c1ccccc1 10.1021/jm970721h
46885226 7974 0 None -18620 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 313 8 1 3 3.3 COc1ccc(OCc2ccccc2)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
CHEMBL1091160 7974 0 None -18620 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 313 8 1 3 3.3 COc1ccc(OCc2ccccc2)c(CCCNC(C)=O)c1 10.1016/j.bmcl.2010.02.084
76319554 85044 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 228 2 0 3 2.6 CCC#CCOc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
CHEMBL2268532 85044 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 228 2 0 3 2.6 CCC#CCOc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
137656978 159204 0 None -147 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 294 4 1 2 3.1 CCC(=O)NC1Cc2ccccc2N(Cc2ccccc2)C1 10.1021/acs.jmedchem.8b00359
CHEMBL4105125 159204 0 None -147 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 294 4 1 2 3.1 CCC(=O)NC1Cc2ccccc2N(Cc2ccccc2)C1 10.1021/acs.jmedchem.8b00359
162644724 178804 0 None -57 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 321 5 1 4 3.0 COc1ccc2nc(-c3ccccc3)nc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
CHEMBL4739898 178804 0 None -57 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 321 5 1 4 3.0 COc1ccc2nc(-c3ccccc3)nc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
46884554 8199 0 None -128 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 313 8 1 3 3.3 COc1cc(CCCNC(C)=O)ccc1OCc1ccccc1 10.1016/j.bmcl.2010.02.084
CHEMBL1092647 8199 0 None -128 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 313 8 1 3 3.3 COc1cc(CCCNC(C)=O)ccc1OCc1ccccc1 10.1016/j.bmcl.2010.02.084
44389864 63990 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 380 10 2 2 4.7 CCNC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL181192 63990 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 380 10 2 2 4.7 CCNC(=O)NCCCc1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
11165283 122603 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 392 9 2 2 4.8 CCNC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
CHEMBL361206 122603 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatoninBinding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin
ChEMBL 392 9 2 2 4.8 CCNC(=O)NC[C@@H]1C[C@H]1c1cccc2c1C[C@@H](CCCCc1ccccc1)O2 10.1016/j.bmcl.2005.01.015
22718561 17058 0 None -3 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 246 5 1 3 2.5 CCc1nc2cccc(CCCNC(C)=O)c2o1 10.1016/j.bmcl.2004.04.082
CHEMBL125665 17058 0 None -3 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 246 5 1 3 2.5 CCc1nc2cccc(CCCNC(C)=O)c2o1 10.1016/j.bmcl.2004.04.082
52918080 60425 0 None -13 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 287 4 1 4 2.1 COc1ccc2c3c(n(CCNC(C)=O)c2n1)CCCC3 10.1016/j.bmcl.2011.02.097
CHEMBL1760957 60425 0 None -13 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 287 4 1 4 2.1 COc1ccc2c3c(n(CCNC(C)=O)c2n1)CCCC3 10.1016/j.bmcl.2011.02.097
127038130 136087 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 347 8 1 2 4.5 CC(=O)NCCc1cccc2ccc(OCCCc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3739824 136087 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 347 8 1 2 4.5 CC(=O)NCCc1cccc2ccc(OCCCc3ccccc3)cc12 10.1039/C5MD00190K
127038132 136278 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 361 9 1 2 4.9 CC(=O)NCCc1cccc2ccc(OCCCCc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3741561 136278 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 361 9 1 2 4.9 CC(=O)NCCc1cccc2ccc(OCCCCc3ccccc3)cc12 10.1039/C5MD00190K
145992795 166227 0 None -29 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 342 5 2 2 3.9 CCCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4284223 166227 0 None -29 2 Human 8.1 pKi = 8.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 342 5 2 2 3.9 CCCNC(=S)NCC1(C)CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
18007928 8562 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 485 12 2 4 5.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CC(=O)O)c4c3)cc12 10.1016/j.bmc.2010.04.008
CHEMBL1095504 8562 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 485 12 2 4 5.5 CC(=O)NCCc1cccc2ccc(OCCCCOc3ccc4cccc(CC(=O)O)c4c3)cc12 10.1016/j.bmc.2010.04.008
49865322 15708 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 267 7 1 3 3.1 CCCC(=O)NCC(C)Sc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
CHEMBL1223196 15708 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 267 7 1 3 3.1 CCCC(=O)NCC(C)Sc1cccc(OC)c1 10.1016/j.bmc.2010.06.100
53238181 919 0 None -741 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 339 5 1 2 4.4 CC(=O)NCCC1=C(CC2CCCCC2)Cc2c1c1CCOc1cc2 10.1021/jm200221q
7780 919 0 None -741 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 339 5 1 2 4.4 CC(=O)NCCC1=C(CC2CCCCC2)Cc2c1c1CCOc1cc2 10.1021/jm200221q
CHEMBL1774519 919 0 None -741 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 339 5 1 2 4.4 CC(=O)NCCC1=C(CC2CCCCC2)Cc2c1c1CCOc1cc2 10.1021/jm200221q
59145848 185475 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 271 3 1 3 2.5 CC(=O)NCCC1CCc2ccn3nc(C)c(C)c3c21 10.1021/acs.jmedchem.0c01836
CHEMBL4871181 185475 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 271 3 1 3 2.5 CC(=O)NCCC1CCc2ccn3nc(C)c(C)c3c21 10.1021/acs.jmedchem.0c01836
127038132 136278 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 361 9 1 2 4.9 CC(=O)NCCc1cccc2ccc(OCCCCc3ccccc3)cc12 10.1039/C5MD00190K
CHEMBL3741561 136278 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 361 9 1 2 4.9 CC(=O)NCCc1cccc2ccc(OCCCCc3ccccc3)cc12 10.1039/C5MD00190K
44424017 84885 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 592 14 4 8 3.4 COc1ccc2[nH]c(C(=O)OCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
CHEMBL226112 84885 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 592 14 4 8 3.4 COc1ccc2[nH]c(C(=O)OCCCOC(=O)c3[nH]c4ccc(OC)cc4c3CCNC(C)=O)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2007.03.080
21581653 137502 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 2 3 1.3 COc1cc2c(CCNC(C)=O)c[nH]c2cn1 10.1016/j.ejmech.2016.01.008
CHEMBL3765249 137502 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 2 3 1.3 COc1cc2c(CCNC(C)=O)c[nH]c2cn1 10.1016/j.ejmech.2016.01.008
25022429 187556 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 393 7 3 4 2.8 COc1ccc2[nH]c(CN3c4ccccc4C[C@H]3CO)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.07.012
CHEMBL498493 187556 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 393 7 3 4 2.8 COc1ccc2[nH]c(CN3c4ccccc4C[C@H]3CO)c(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.07.012
44349108 16670 0 None -2 2 Human 8.0 pKi = 8 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 246 6 1 3 2.7 CCCC(=O)NCCCc1cccc2ncoc12 10.1016/j.bmcl.2004.04.082
CHEMBL124914 16670 0 None -2 2 Human 8.0 pKi = 8 Binding
Binding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligandBinding affinity against human Melatonin receptor type 1A by using 2-[125I]iodomelatonin as radioligand
ChEMBL 246 6 1 3 2.7 CCCC(=O)NCCCc1cccc2ncoc12 10.1016/j.bmcl.2004.04.082
127025783 137200 0 None -4 2 Human 8.0 pKi = 8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3occ(CNC(=O)CF)c3c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL3759160 137200 0 None -4 2 Human 8.0 pKi = 8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 287 4 1 3 3.2 COc1ccc2ccc3occ(CNC(=O)CF)c3c2c1 10.1016/j.ejmech.2015.12.047
137633385 155860 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human melatonin MT1 assessed as inhibition constantBinding affinity to human melatonin MT1 assessed as inhibition constant
ChEMBL 311 4 0 1 4.8 O=C(c1ccc(F)cc1)N(Cc1ccccc1)C1CCCCC1 10.1021/acs.jmedchem.1c01571
CHEMBL4066660 155860 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human melatonin MT1 assessed as inhibition constantBinding affinity to human melatonin MT1 assessed as inhibition constant
ChEMBL 311 4 0 1 4.8 O=C(c1ccc(F)cc1)N(Cc1ccccc1)C1CCCCC1 10.1021/acs.jmedchem.1c01571
CHEMBL5200484 155860 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human melatonin MT1 assessed as inhibition constantBinding affinity to human melatonin MT1 assessed as inhibition constant
ChEMBL 311 4 0 1 4.8 O=C(c1ccc(F)cc1)N(Cc1ccccc1)C1CCCCC1 10.1021/acs.jmedchem.1c01571
1348 1807 1 None -100 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10.1021/jm401343c
44208891 1807 1 None -100 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10.1021/jm401343c
CHEMBL3260983 1807 1 None -100 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10.1021/jm401343c
54582195 60423 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 329 5 1 5 1.9 COc1ccc2c(C(=O)C(F)(F)F)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760955 60423 0 None -3 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 329 5 1 5 1.9 COc1ccc2c(C(=O)C(F)(F)F)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
16094583 165576 3 None -69 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 291 5 1 1 4.0 O=C(NCC=C(c1ccccc1)c1ccccc1)C1CCC1 10.1021/jm060850a
CHEMBL426168 165576 3 None -69 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 291 5 1 1 4.0 O=C(NCC=C(c1ccccc1)c1ccccc1)C1CCC1 10.1021/jm060850a
11418246 62059 0 None -4 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 6 1 3 5.8 O=C(NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12)C1CCC1 10.1016/j.ejmech.2011.02.044
CHEMBL1779806 62059 0 None -4 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 403 6 1 3 5.8 O=C(NCCc1c(Sc2ccc(F)cc2)sc2ccc(F)cc12)C1CCC1 10.1016/j.ejmech.2011.02.044
44264909 203513 0 None -117 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 293 5 1 2 4.8 CCCC(=O)Nc1ccc(Cc2cccc3occc23)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7875 203513 0 None -117 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 293 5 1 2 4.8 CCCC(=O)Nc1ccc(Cc2cccc3occc23)cc1 10.1016/j.bmcl.2003.11.030
44264942 203723 0 None -19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 313 5 1 4 4.0 CCCC(=O)Nc1ccc(Oc2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL8032 203723 0 None -19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 313 5 1 4 4.0 CCCC(=O)Nc1ccc(Oc2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2003.11.030
10390684 11210 0 None -4 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 359 9 1 3 3.0 CCC(=O)NCCc1c(OCC[N+](C)(C)C)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
CHEMBL1179488 11210 0 None -4 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 359 9 1 3 3.0 CCC(=O)NCCc1c(OCC[N+](C)(C)C)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
CHEMBL78338 11210 0 None -4 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 359 9 1 3 3.0 CCC(=O)NCCc1c(OCC[N+](C)(C)C)ccc2ccc(OC)cc12 10.1016/S0960-894X(97)00444-7
16094585 82463 0 None -204 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 321 6 1 2 4.0 COc1cccc(/C(=C/CNC(=O)C2CCC2)c2ccccc2)c1 10.1021/jm060850a
CHEMBL218065 82463 0 None -204 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells
ChEMBL 321 6 1 2 4.0 COc1cccc(/C(=C/CNC(=O)C2CCC2)c2ccccc2)c1 10.1021/jm060850a
54583161 60421 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 452 8 1 6 3.4 COc1ccc2c(CN3CCC(C(=O)c4ccc(F)cc4)CC3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
CHEMBL1760953 60421 0 None -1 2 Human 5.0 pKi = 5.0 Binding
Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 452 8 1 6 3.4 COc1ccc2c(CN3CCC(C(=O)c4ccc(F)cc4)CC3)cn(CCNC(C)=O)c2n1 10.1016/j.bmcl.2011.02.097
44429454 148671 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 336 7 2 2 4.3 CCCC(=O)NCCc1c[nH]c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
CHEMBL394408 148671 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 336 7 2 2 4.3 CCCC(=O)NCCc1c[nH]c2c(-c3ccccc3)cc(OC)cc12 10.1016/j.bmc.2007.04.013
44264962 203132 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 5 1 3 4.0 C/C=C/C(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
CHEMBL7559 203132 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 5 1 3 4.0 C/C=C/C(=O)Nc1ccc(Oc2cccc(OC)c2)cc1 10.1016/j.bmcl.2003.11.030
18702059 203278 3 None -7 2 Human 7.0 pKi = 7 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 5 1 3 3.8 COc1cccc(Oc2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL7673 203278 3 None -7 2 Human 7.0 pKi = 7 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 5 1 3 3.8 COc1cccc(Oc2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
145979282 166111 0 None -16 3 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
CHEMBL4281915 166111 0 None -16 3 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 300 3 2 2 3.0 CNC(=S)NCC1CCc2ccc3ccc(OC)cc3c21 10.1016/j.ejmech.2017.10.025
1357 2440 133 None -1 9 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10696085
1672 2440 133 None -1 9 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10696085
224 2440 133 None -1 9 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10696085
896 2440 133 None -1 9 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10696085
CHEMBL45 2440 133 None -1 9 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10696085
DB01065 2440 133 None -1 9 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10696085
1357 2440 133 125I-Iodomelatonin -1 9 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
198 310 120 125I-Iodomelatonin -1 6 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 125I-Iodomelatonin -1 6 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 125I-Iodomelatonin -1 6 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 125I-Iodomelatonin -1 6 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 125I-Iodomelatonin -1 6 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Mel -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Mel -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Mel -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Mel -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Mel -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Mel -1 9 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1349 1811 0 125I-Iodomelatonin -1 2 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 None
5311134 1811 0 125I-Iodomelatonin -1 2 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Mel -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Mel -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Mel -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Mel -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Mel -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Mel -1 9 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
4004 214319 0 35S-GTPGammaS - 1 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 330 9 0 8 2.1 CCOC(=O)CC(C(=O)OCC)SP(=S)(OC)OC None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
198 310 120 125I-Mel -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 125I-Mel -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 125I-Mel -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 125I-Mel -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 125I-Mel -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
198 310 120 125I-Iodomelatonin -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 125I-Iodomelatonin -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 125I-Iodomelatonin -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 125I-Iodomelatonin -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 125I-Iodomelatonin -1 6 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Mel -1 9 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Mel -1 9 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Mel -1 9 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Mel -1 9 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Mel -1 9 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Mel -1 9 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
198 310 120 None -1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 None -1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 None -1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 None -1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 None -1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
1356 3224 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
208902 3224 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
2355 3224 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
CHEMBL1218 3224 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
DB00980 3224 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
5 139 66 125I-Mel -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-Mel -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-Mel -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-Mel -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 141 116 125I-Iodomelatonin -14791 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 125I-Iodomelatonin -14791 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 125I-Iodomelatonin -14791 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
4209 3102 71 125I-Mel -63095 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3102 71 125I-Mel -63095 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3102 71 125I-Mel -63095 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3102 71 125I-Mel -63095 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3102 71 125I-Mel -63095 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3102 71 125I-Mel -63095 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
122162 2345 67 125I-Iodomelatonin -18 2 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1363 2345 67 125I-Iodomelatonin -18 2 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
CHEMBL286615 2345 67 125I-Iodomelatonin -18 2 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
70547 112831 72 125I-Iodomelatonin -10 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
CHEMBL33171 112831 72 125I-Iodomelatonin -10 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
1349 1811 0 125I-Iodomelatonin -1 2 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 None
5311134 1811 0 125I-Iodomelatonin -1 2 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 None
164157684 214322 0 125I-Iodomelatonin -60 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 1094 24 4 18 8.7 CC(C)(C)OC(=O)N(C)CC(CN(C)C(=O)OC(C)(C)C)CSP(=O)(O)O.CNCC(CNC)CSP(=O)(OCOC(=O)C1=CC=CC=C1)OCOC(=O)C2=CC=CC=C2.C1=CC=C(C=C1)C(=O)OCCl None
903 112389 83 125I-Iodomelatonin 1 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
CHEMBL33103 112389 83 125I-Iodomelatonin 1 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
122162 2345 67 125I-Iodomelatonin -18 2 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1363 2345 67 125I-Iodomelatonin -18 2 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
CHEMBL286615 2345 67 125I-Iodomelatonin -18 2 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1357 2440 133 125I-Iodomelatonin -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Iodomelatonin -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Iodomelatonin -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Iodomelatonin -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Iodomelatonin -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Iodomelatonin -1 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1358 124 35 125I-Iodomelatonin -870 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 None
3976006 124 35 125I-Iodomelatonin -870 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 None
CHEMBL285718 124 35 125I-Iodomelatonin -870 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 None
None 214318 0 125I-Iodomelatonin -1 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 218 2 2 4 1.5 CC(=O)N1C=C(C2=C1C=CC(=C2)O)CCN None
None 214318 0 35S-GTPGammaS -1 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 218 2 2 4 1.5 CC(=O)N1C=C(C2=C1C=CC(=C2)O)CCN None
681 1432 65 None -38 39 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1432 65 None -38 39 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1432 65 None -38 39 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1432 65 None -38 39 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1432 65 None -38 39 Human 8.3 pKi = 8.3 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
12835 214323 0 125I-Iodomelatonin -6 2 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 191 3 2 2 1.7 COC1=CC2=C(C=C1)NC=C2CCO None
122162 2345 67 125I-Iodomelatonin -18 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1363 2345 67 125I-Iodomelatonin -18 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
CHEMBL286615 2345 67 125I-Iodomelatonin -18 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1357 2440 133 125I-Mel -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2440 133 125I-Mel -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2440 133 125I-Mel -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2440 133 125I-Mel -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2440 133 125I-Mel -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2440 133 125I-Mel -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
903 112389 83 125I-Iodomelatonin 1 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
CHEMBL33103 112389 83 125I-Iodomelatonin 1 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
70547 112831 72 125I-Iodomelatonin -10 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
CHEMBL33171 112831 72 125I-Iodomelatonin -10 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
10220503 3687 0 None -2 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 None
4820 3687 0 None -2 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 None
7393 3687 0 None -2 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 None
CHEMBL2103822 3687 0 None -2 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 None
DB09071 3687 0 None -2 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 None
None 214318 0 125I-Mel -1 2 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 218 2 2 4 1.5 CC(=O)N1C=C(C2=C1C=CC(=C2)O)CCN None
198 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
198 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
82148 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
82148 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
99 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
99 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
CHEMBL10878 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
CHEMBL10878 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
DB06594 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
DB06594 310 120 None -1 6 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
24954989 1497 1 None 6 2 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 21568291
7774 1497 1 None 6 2 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 21568291
CHEMBL1802025 1497 1 None 6 2 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 21568291
71533431 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 23265885
7775 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 23265885
CHEMBL2314259 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 23265885
57381112 1383 0 None 20 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 22301214
7776 1383 0 None 20 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 22301214
CHEMBL1946221 1383 0 None 20 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 22301214
115348 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
115348 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
1343 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
1343 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
CHEMBL289233 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
CHEMBL289233 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
DB08190 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
DB08190 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
1356 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
208902 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
2355 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
CHEMBL1218 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
DB00980 3224 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
11196 1947 0 None -3 2 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 888 18 3 11 5.9 COc1ccc2c(n1)c(CCNC(=O)C)cn2CCNC(=O)CCCCCN1c2ccc(cc2C(/C/1=C\C=C\C1=[N+](CC)c2c(C1(C)C)cc(cc2)S(=O)(=O)O)(C)C)S(=O)(=O)[O-] 28493341
154699456 1947 0 None -3 2 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 888 18 3 11 5.9 COc1ccc2c(n1)c(CCNC(=O)C)cn2CCNC(=O)CCCCCN1c2ccc(cc2C(/C/1=C\C=C\C1=[N+](CC)c2c(C1(C)C)cc(cc2)S(=O)(=O)O)(C)C)S(=O)(=O)[O-] 28493341
122162 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10696085
122162 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 12764576
122162 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 2843633
122162 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 9089668
1363 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10696085
1363 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 12764576
1363 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 2843633
1363 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 9089668
CHEMBL286615 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10696085
CHEMBL286615 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 12764576
CHEMBL286615 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 2843633
CHEMBL286615 2345 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 9089668
7773 3840 0 None -12 2 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 296 3 2 2 2.6 COc1ccc2c(c1)C(CNC(=O)N)Cc1c(C2)cccc1 17907131
86277838 3840 0 None -12 2 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 296 3 2 2 2.6 COc1ccc2c(c1)C(CNC(=O)N)Cc1c(C2)cccc1 17907131
11185529 3839 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 15293992
11185529 3839 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 17907131
7772 3839 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 15293992
7772 3839 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 17907131
CHEMBL189449 3839 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 15293992
CHEMBL189449 3839 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 17907131
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 12764576
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 2991499
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9089668
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9618428
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 12764576
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 2991499
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9089668
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9618428
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 12764576
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 2991499
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9089668
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9618428
24763223 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 22927210
8289 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 22927210
CHEMBL3260987 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 22927210
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10696085
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 2991499
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9089668
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9618428
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10696085
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 2991499
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9089668
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9618428
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10696085
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 2991499
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9089668
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9618428
24750192 3842 10 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 18052314
7777 3842 10 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 18052314
CHEMBL237236 3842 10 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 18052314
12324 3836 0 None 2 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 591 13 3 4 7.0 O=C(C)NCCc1c(Br)[nH]c2c1cc(cc2)OCCCCCCNC(=O)Oc1cc(ccc1)c1ccccc1 30126274
145966622 3836 0 None 2 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 591 13 3 4 7.0 O=C(C)NCCc1c(Br)[nH]c2c1cc(cc2)OCCCCCCNC(=O)Oc1cc(ccc1)c1ccccc1 30126274
CHEMBL4210086 3836 0 None 2 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 591 13 3 4 7.0 O=C(C)NCCc1c(Br)[nH]c2c1cc(cc2)OCCCCCCNC(=O)Oc1cc(ccc1)c1ccccc1 30126274
7778 799 0 None 97 2 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 20444610
9957516 799 0 None 97 2 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 20444610
CHEMBL1094546 799 0 None 97 2 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 12 2 4 6.1 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc(cc1)c1ccc(cc1)C(=O)O)cc2 20444610
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12764576
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 2991499
1357 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 9089668
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12764576
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 2991499
1672 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 9089668
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12764576
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 2991499
224 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 9089668
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12764576
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 2991499
896 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 9089668
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12764576
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 2991499
CHEMBL45 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 9089668
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 12764576
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 2991499
DB01065 2440 133 None -1 9 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 9089668
10220503 3687 0 None -2 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 19054552
4820 3687 0 None -2 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 19054552
7393 3687 0 None -2 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 19054552
CHEMBL2103822 3687 0 None -2 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 19054552
DB09071 3687 0 None -2 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 4 1 2 2.3 CCC(=O)NC[C@@H]1C[C@H]1c1cccc2c1CCO2 19054552
4004 214319 0 None - 1 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 330 9 0 8 2.1 CCOC(=O)CC(C(=O)OCC)SP(=S)(OC)OC None
1351 2353 15 None -1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 15302228
219018 2353 15 None -1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 15302228
CHEMBL4079759 2353 15 None -1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 15302228
127856 3366 0 None -3 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 4 1 1 3.3 O=C(C1CCC1)NCCc1cccc2c1cccc2 12764576
1360 3366 0 None -3 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 4 1 1 3.3 O=C(C1CCC1)NCCc1cccc2c1cccc2 12764576
CHEMBL12296 3366 0 None -3 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 4 1 1 3.3 O=C(C1CCC1)NCCc1cccc2c1cccc2 12764576
1358 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 12764576
1358 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9089668
1358 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9737724
3976006 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 12764576
3976006 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9089668
3976006 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9737724
CHEMBL285718 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 12764576
CHEMBL285718 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9089668
CHEMBL285718 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9737724
1348 1807 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10205014
1348 1807 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 9089668
44208891 1807 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10205014
44208891 1807 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 9089668
CHEMBL3260983 1807 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10205014
CHEMBL3260983 1807 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 9089668
1354 3369 10 None -275 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 12764576
22133318 3369 10 None -275 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 12764576
CHEMBL490188 3369 10 None -275 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 12764576
1359 2130 20 None -125 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10737738
5311198 2130 20 None -125 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10737738
CHEMBL274438 2130 20 None -125 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10737738
1353 3368 3 None -112 2 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 12764576
9998187 3368 3 None -112 2 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 12764576
CHEMBL33549 3368 3 None -112 2 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 12764576
10849065 137 8 None 4 2 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 11068946
1345 137 8 None 4 2 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 11068946
CHEMBL126809 137 8 None 4 2 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 11068946
1361 3367 0 None -1 2 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 4 1 2 3.1 CCc1ccc2c(c1)c(CCNC(=O)C)cs2 12764576
9816339 3367 0 None -1 2 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 4 1 2 3.1 CCc1ccc2c(c1)c(CCNC(=O)C)cs2 12764576
1350 1951 0 None -95 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10737738
4172142 1951 0 None -95 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10737738
CHEMBL10009 1951 0 None -95 3 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 348 6 1 3 4.1 CCCC(=O)NCCc1c2c3ccccc3Cn2c2c1cc(OC)cc2 10737738
1362 3370 18 None 39 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
9870523 3370 18 None 39 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
CHEMBL429392 3370 18 None 39 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
1355 3371 3 None 70 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
9806449 3371 3 None 70 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
CHEMBL14453 3371 3 None 70 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
1349 1811 0 None -1 2 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 10696085
1349 1811 0 None -1 2 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 9618428
5311134 1811 0 None -1 2 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 10696085
5311134 1811 0 None -1 2 Human 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 3 1 3 1.1 CC(=O)NCCN1CCc2c1c1CCOc1cc2 9618428