Ligand source activities (1 row/activity)





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DOI

57781216 125847 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 125847 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 1532 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 1532 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 1532 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 184831 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 184831 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 184597 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 184597 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 184858 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 184858 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 185329 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 185329 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 185004 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 185004 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 186267 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 186267 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 166667 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 166667 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 185296 18 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 185296 18 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 184831 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 184831 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 186333 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 186333 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 100116 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 100116 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 184597 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 184597 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
198 313 126 None -3 4 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 313 126 None -3 4 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
99 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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 166475 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 166475 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 166751 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 166751 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 185004 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 185004 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 185011 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 185011 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 185839 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 185839 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 185296 18 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 185296 18 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 190229 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 190229 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 184858 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 184858 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 185329 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 185329 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 186267 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 186267 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 192518 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 192518 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 62019 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 62019 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 192518 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 192518 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 66927 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 66927 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 190147 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 190147 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 185944 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 185944 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 159520 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 159520 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 166490 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 166490 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 167281 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 167281 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 123163 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 123163 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 184447 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 184447 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 186142 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 186142 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 137684 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 137684 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 137820 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 137820 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 190147 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 190147 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
198 313 126 None -3 4 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 313 126 None -3 4 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
99 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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
198 313 126 None -3 4 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
198 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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
99 313 126 None -3 4 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
99 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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
198 313 126 None -3 4 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 313 126 None -3 4 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
99 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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
198 313 126 None -3 4 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 313 126 None -3 4 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
99 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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
198 313 126 None -3 4 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 313 126 None -3 4 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
99 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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 123162 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 123162 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 185011 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 185011 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 8890 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 8890 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 166675 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 166675 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 167219 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 167219 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 159675 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 159675 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 166791 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 166791 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 166912 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 166912 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 156377 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 156377 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 8843 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 8843 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 123148 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 123148 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 28915 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 28915 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 8643 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 8643 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 60752 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 60752 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 112236 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 112236 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 190229 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 190229 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 167057 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 167057 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 60764 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 60764 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 8868 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 8868 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 87074 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 87074 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 123147 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 123147 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 156852 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 156852 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 43220 42 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 43220 42 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 3909 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 3909 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 3909 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 62408 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 62408 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 157944 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 157944 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 157118 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 157118 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 123154 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 123154 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 166497 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 166497 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 123165 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 123165 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 60755 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 60755 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 184447 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 184447 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 8521 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 8521 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 8671 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 8671 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 8889 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 8889 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 8644 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 8644 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 87075 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 87075 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 167032 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 167032 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 167120 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 167120 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 156246 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 156246 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 62401 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 62401 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 121320 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 121320 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 112322 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 112322 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 8645 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 8645 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 190970 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 190970 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 8666 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 8666 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 62400 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 62400 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 123143 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 123143 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 123145 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 123145 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 207977 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 207977 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 158895 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 158895 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 49 None -144 11 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 49 None -144 11 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 49 None -144 11 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 49 None -144 11 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 105219 94 None -1 4 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 105219 94 None -1 4 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 814 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 814 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 814 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 180732 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 180732 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
198 313 126 None -3 4 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 313 126 None -3 4 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
99 313 126 None -3 4 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 313 126 None -3 4 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 313 126 None -3 4 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 123146 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 123146 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 121317 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 121317 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 137738 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 137738 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 166557 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 166557 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 62028 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 62028 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 8665 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 8665 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 185395 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 185395 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 167371 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 167371 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 157505 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 157505 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 123153 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 123153 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 60763 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 60763 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 180075 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 180075 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 121328 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 121328 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 123152 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 123152 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 3435 5 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 3435 5 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 3435 5 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 121318 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 121318 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 157463 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 157463 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 123149 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 123149 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 166611 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 166611 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 60753 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 60753 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 934 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 934 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 934 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 137819 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 137819 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 137634 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 137634 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 705 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 705 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 705 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 182758 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 182758 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 180922 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 180922 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 8565 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 8565 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 159073 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 159073 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 112334 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 112334 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 166557 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 166557 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 166929 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 166929 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 167236 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 167236 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 60754 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 60754 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 137800 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 137800 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 121319 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 121319 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 166623 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 166623 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 123166 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 123166 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 157512 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 157512 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 180138 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 180138 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 137689 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 137689 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 8715 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 8715 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 166431 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 166431 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 121323 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 121323 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 29900 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 29900 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 3438 5 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 3438 5 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 3438 5 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 137849 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 137849 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 158179 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 158179 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 166675 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 166675 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 137731 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 137731 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 87073 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 87073 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 123167 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 123167 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 167190 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 167190 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 87071 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 87071 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 8716 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 8716 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 137733 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 137733 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 156086 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 156086 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 158885 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 158885 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 123142 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 123142 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 74146 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 74146 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 60762 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 60762 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 121325 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 121325 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 121321 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 121321 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 195700 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 195700 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 110867 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 110867 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 216 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 216 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 216 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 60753 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 60753 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 3914 5 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 3914 5 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 3914 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 2485 139 None 1 5 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 3919 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 3919 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 3920 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 3920 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 3918 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 3918 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 554 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 554 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 554 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 554 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




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10440 2680 20 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 2680 20 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 2680 20 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 121328 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 121328 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 30966 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 30966 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 112322 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 112322 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 125852 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 125852 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 125850 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 125850 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 125854 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 125854 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 125847 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 125847 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 125844 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 125844 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 160836 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 160836 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 125860 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 125860 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 125849 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 125849 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 125846 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 125846 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 125853 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 125853 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 9774 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 9774 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 161567 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 161567 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 160964 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 160964 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 125859 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 125859 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 160833 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 160833 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 98229 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 98229 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 116787 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 116787 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 160830 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 160830 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 125856 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 125856 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 125858 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 125858 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 109823 5 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 109823 5 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 125857 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 125857 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 28803 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 28803 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 28942 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 28942 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 109691 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 109691 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 175023 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 175023 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 125845 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 125845 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 47 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 47 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 47 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 47 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 29320 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 29320 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 141962 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 141962 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 8250 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 8250 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 9747 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 9747 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 9842 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 9842 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 162751 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 162751 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 109823 5 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 109823 5 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 8037 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 8037 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 29851 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 29851 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 138660 7 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 138660 7 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 9724 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 9724 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 29287 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 29287 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 118740 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 118740 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 188714 42 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 188714 42 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 9403 4 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 9403 4 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 28749 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 28749 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 119156 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 119156 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 188714 42 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 188714 42 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 29395 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 29395 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 118870 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 118870 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 165048 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 165048 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 28917 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 28917 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 29303 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 29303 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 29492 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 29492 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 29537 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 29537 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 30250 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 30250 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 30634 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 30634 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 31705 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 31705 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 119251 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 119251 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 100202 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 100202 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 119221 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 119221 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 125851 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 125851 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 69828 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 69828 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 30408 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 30408 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 30715 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 30715 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 116533 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 116533 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 119006 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 119006 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 119429 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 119429 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 193107 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 193107 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 28891 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 28891 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 28915 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 28915 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 32049 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 32049 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 119378 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 119378 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 165256 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 165256 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 26862 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 26862 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 29679 4 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 29679 4 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 125848 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 125848 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 9866 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 9866 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 28931 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 28931 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 28989 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 28989 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 29011 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 29011 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 29190 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 29190 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 161671 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 161671 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 69493 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 69493 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 26708 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 26708 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 27417 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 27417 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 170436 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 170436 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 29862 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 29862 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 33201 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 33201 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 119143 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 119143 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 119400 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 119400 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 168455 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 168455 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 29164 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 29164 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 30168 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 30168 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 32798 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 32798 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 67258 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 67258 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 10091 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 10091 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 188786 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 188786 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 125855 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 125855 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 28892 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 28892 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 29525 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 29525 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 29900 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 29900 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 29902 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 29902 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 30059 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 30059 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 119444 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 119444 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 27418 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 27418 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 29357 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 29357 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 32902 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 32902 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 120015 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 120015 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 110866 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 110866 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 29914 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 29914 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 138239 6 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 138239 6 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 99019 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 99019 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 67006 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 67006 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 9419 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 9419 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 30173 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 30173 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 31598 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 31598 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 30643 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 30643 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 119326 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 119326 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 136344 3 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 136344 3 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
9064 105219 94 None - 0 Human 4.6 pIC50 = 4.6 Binding
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cellsAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells
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.bmc.2021.116270
CHEMBL311498 105219 94 None - 0 Human 4.6 pIC50 = 4.6 Binding
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cellsAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells
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.bmc.2021.116270
18175032 175596 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 175596 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 187372 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 187372 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 31707 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 31707 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 32407 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 32407 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 168606 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 168606 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 109204 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 109204 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 115490 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 115490 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 116756 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 116756 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 169319 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 169319 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 175495 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 175495 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 30710 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 30710 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 31396 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 31396 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 9798 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 9798 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 30303 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 30303 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 119427 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 119427 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 187559 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 187559 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 8437 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 8437 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 29613 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 29613 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 30792 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 30792 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 31604 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 31604 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 116794 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 116794 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 118747 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 118747 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 100081 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 100081 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 71705 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 71705 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 175699 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 175699 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 9304 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 9304 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 28840 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 28840 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 29457 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 29457 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 29836 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 29836 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 108565 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 108565 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 29948 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 29948 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 118798 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 118798 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 119042 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 119042 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 119283 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 119283 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 119373 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 119373 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 60079 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 60079 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 29506 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 29506 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 29740 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 29740 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 30076 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 30076 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 32137 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 32137 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 33219 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 33219 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 66898 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 66898 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 187370 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 187370 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 192655 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 192655 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 9433 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 9433 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 30165 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 30165 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 30626 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 30626 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 125807 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 125807 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 29167 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 29167 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 119146 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 119146 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 31775 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 31775 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 32518 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 32518 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 116788 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 116788 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 32059 4 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 32059 4 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 33096 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 33096 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 168219 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 168219 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 29582 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 29582 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 116402 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 116402 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 118977 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 118977 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 119043 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 119043 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 119343 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 119343 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 174984 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 174984 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 30066 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 30066 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 31708 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 31708 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 32888 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 32888 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 118778 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 118778 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 30880 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 30880 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 119340 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 119340 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 30245 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 30245 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 187695 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 187695 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 61405 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 61405 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2680 20 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 2680 20 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 2680 20 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
9903515 22793 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 22793 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 100116 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 100116 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 112580 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 112580 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 100116 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 100116 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 116436 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 116436 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 62015 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 62015 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 47 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 47 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 47 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 47 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 116575 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 116575 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 118153 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 118153 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 106878 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 106878 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 62014 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 62014 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 23563 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 23563 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 63797 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 63797 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 185895 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 185895 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 35839 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 35839 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 19845 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 19845 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 123162 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 123162 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 125847 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 125847 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 62017 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 62017 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 125853 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 125853 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 63795 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 63795 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 207565 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 207565 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 64989 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 64989 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 138075 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 138075 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 86414 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 86414 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 63796 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 63796 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 62013 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 62013 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 32712 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 32712 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 98156 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 98156 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 205618 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 205618 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 67600 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 67600 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 78789 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 78789 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 78794 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 78794 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 78798 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 78798 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 78799 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 78799 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 78800 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 78800 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 78804 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 78804 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 1416 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 1416 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 1416 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 1416 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 1416 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 1416 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 19485 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 19485 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 62025 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 62025 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 86412 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 86412 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 1532 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 1532 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 1532 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 125846 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 125846 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 125849 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 125849 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 47 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 47 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 47 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 47 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 62023 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 62023 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 116654 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 116654 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 8644 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 8644 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 2395 21 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 2395 21 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 2395 21 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 30961 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 30961 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 47 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 47 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 47 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 47 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 101791 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 101791 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 63792 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 63792 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 63794 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 63794 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 8521 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 8521 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 100610 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 100610 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 100610 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 100610 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 20256 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 20256 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 22252 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 22252 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 166475 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 166475 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 86415 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 86415 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 21363 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 21363 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 62016 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 62016 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 20195 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 20195 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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+
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 67323 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 67323 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 27077 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 27077 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 109823 5 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 109823 5 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 171792 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 171792 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 109823 5 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 109823 5 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 109823 5 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 109823 5 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 63793 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 63793 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 186315 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 186315 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 119286 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 119286 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 98913 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 98913 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 19484 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 19484 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 20704 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 20704 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 167879 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 167879 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 60752 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 60752 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 186272 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 186272 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 137911 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 137911 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 138060 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 138060 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 86417 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 86417 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 116628 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 116628 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 98602 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 98602 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 125856 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 125856 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 60752 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 60752 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 60752 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 60752 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 8715 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 8715 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 166497 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 166497 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 167281 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 167281 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 159520 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 159520 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 185919 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 185919 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 86410 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 86410 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 193857 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 193857 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 63799 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 63799 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 184858 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 184858 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 67526 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 67526 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 186176 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 186176 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 19845 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 19845 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 168324 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 168324 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 8645 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 8645 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 186333 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 186333 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 205506 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 205506 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 125857 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 125857 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 166557 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 166557 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 166667 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 166667 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 19835 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 19835 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 185329 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 185329 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 21363 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 21363 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 125845 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 125845 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 125858 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 125858 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 63798 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 63798 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 3437 22 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 3437 22 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 3437 22 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 3437 22 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 3437 22 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 3437 22 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 3437 22 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 3437 22 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 3437 22 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 814 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 814 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 814 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 3438 5 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 3438 5 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 3438 5 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 3438 5 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 3438 5 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 3438 5 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 67327 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 67327 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 3438 5 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 3438 5 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 3438 5 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 166557 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 166557 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 167022 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 167022 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 167236 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 167236 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 3438 5 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 3438 5 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 3438 5 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 157944 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 157944 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 186267 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 186267 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 114811 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 114811 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 114811 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 114811 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 8843 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 8843 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 27118 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 27118 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 21482 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 21482 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 18549 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 18549 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 123163 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 123163 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 185944 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 185944 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 15879 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 15879 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 207626 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 207626 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 112871 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 112871 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 3911 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 3911 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 3911 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 116811 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 116811 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 8643 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 8643 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 116593 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 116593 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 166611 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 166611 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 166929 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 166929 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 156086 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 156086 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 3917 13 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 3917 13 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 3917 13 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 88553 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 88553 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 184831 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 184831 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 62020 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 62020 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 28953 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 28953 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 8868 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 8868 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 15877 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 15877 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 68676 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 68676 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 20675 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 20675 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 68016 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 68016 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 63002 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 63002 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 122341 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 122341 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 123275 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 123275 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 130170 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 130170 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 205180 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 205180 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 185839 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 185839 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 166623 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 166623 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 166751 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 166751 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 207789 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 207789 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 8867 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 8867 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 118491 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 118491 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 8716 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 8716 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 96997 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 96997 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 184597 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 184597 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 186142 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 186142 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 62018 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 62018 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 62024 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 62024 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 195224 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 195224 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 76702 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 76702 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 216 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 216 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 216 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 30652 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 30652 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 19986 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 19986 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 110868 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 110868 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 185004 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 185004 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 136848 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 136848 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 184563 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 184563 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 78298 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 78298 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 136848 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 136848 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 190229 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 190229 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 112322 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 112322 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 112322 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 112322 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 112322 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 112322 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 67493 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 67493 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 117085 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 117085 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 168547 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 168547 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 116914 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 116914 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 70309 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 70309 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 60755 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 60755 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 185621 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 185621 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 62030 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 62030 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 24737 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 24737 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 115357 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 115357 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 110865 6 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 110865 6 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 67495 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 67495 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 159073 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 159073 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 8889 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 8889 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 60753 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 60753 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 67495 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 67495 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 62029 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 62029 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 174222 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 174222 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 116540 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 116540 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 8666 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 8666 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 157079 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 157079 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 123166 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 123166 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 137898 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 137898 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 78085 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 78085 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 15850 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 15850 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 150223 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 150223 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 195487 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 195487 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 208077 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 208077 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 192518 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 192518 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 116592 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 116592 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 137684 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 137684 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 159675 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 159675 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 20601 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 20601 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 137692 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 137692 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 124407 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 124407 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 87363 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 87363 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 77114 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 77114 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 205225 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 205225 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 29900 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 29900 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 205294 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 205294 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 149244 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 149244 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 174677 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 174677 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 196271 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 196271 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 174677 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 174677 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 41 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 41 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 41 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 60756 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 60756 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 15831 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 15831 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 66289 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 66289 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 205372 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 205372 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 101811 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 101811 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 174924 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 174924 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 174924 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 174924 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 196563 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 196563 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 15851 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 15851 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 66145 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 66145 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 21780 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 21780 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 47 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 47 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 47 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 47 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 47 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 47 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 77317 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 77317 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 136689 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 136689 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 196745 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 196745 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 69075 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 69075 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 64990 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 64990 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 196563 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 196563 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 3437 22 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 3437 22 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 3437 22 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 123679 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 123679 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 109386 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 109386 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 3437 22 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 3437 22 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 3437 22 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 92209 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 92209 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 181443 3 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 181443 3 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 15856 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 15856 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 15934 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 15934 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 208183 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 208183 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 123145 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 123145 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 16522 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 16522 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 77124 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 77124 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 208110 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 208110 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 7705 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 7705 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 16774 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 16774 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 204862 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 204862 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 136689 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 136689 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 164218 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 164218 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 207844 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 207844 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 137988 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 137988 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 189624 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 189624 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 15894 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 15894 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 208337 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 208337 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 83272 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 83272 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 15927 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 15927 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 15933 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 15933 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 189624 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 189624 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 87071 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 87071 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 60759 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 60759 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 123155 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 123155 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 208375 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 208375 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 208375 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 208375 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 159122 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 159122 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 182130 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 182130 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 190629 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 190629 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 89885 1 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 89885 1 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 87748 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 87748 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 181831 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 181831 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 8255 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 8255 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 3913 5 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 3913 5 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 3913 5 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 208104 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 208104 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 194767 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 194767 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 88554 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 88554 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 3913 5 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 3913 5 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 3913 5 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 87365 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 87365 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 116413 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 116413 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 3913 5 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 3913 5 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 3913 5 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 3913 5 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 3913 5 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 3913 5 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 184447 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 184447 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 123143 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 123143 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 123942 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 123942 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 62028 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 62028 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 16888 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 16888 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 96544 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 96544 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 89480 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 89480 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 123149 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 123149 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 175211 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 175211 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 208307 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 208307 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 208307 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 208307 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 87071 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 87071 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 87071 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 87071 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 187114 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 187114 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 15832 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 15832 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 181833 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 181833 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 121317 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 121317 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 87364 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 87364 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 112552 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 112552 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 64453 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 64453 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 207819 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 207819 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 101547 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 101547 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 137809 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 137809 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 170877 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 170877 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 119205 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 119205 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 119205 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 119205 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 170877 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 170877 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 16506 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 16506 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 8419 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 8419 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 188983 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 188983 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 190147 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 190147 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 179887 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 179887 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 98166 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 98166 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 188983 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 188983 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 139451 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 139451 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 196096 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 196096 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 87532 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 87532 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 182331 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 182331 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 166257 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 166257 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 169116 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 169116 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 137849 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 137849 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 137731 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 137731 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 2387 75 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 2387 75 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 2387 75 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 60763 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 60763 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 159332 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 159332 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 66325 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 66325 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 122710 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 122710 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 164613 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 164613 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 88552 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 88552 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 67051 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 67051 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 108500 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 108500 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 108500 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 108500 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 16838 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 16838 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 3909 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 3909 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 3909 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 121319 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 121319 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 137732 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 137732 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 188150 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 188150 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 27516 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 27516 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 121323 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 121323 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 141060 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 141060 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 123164 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 123164 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 4676 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 4676 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 77994 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 77994 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 189727 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 189727 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 205030 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 205030 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 98313 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 98313 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 204983 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 204983 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 189727 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 189727 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 189727 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 189727 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 189727 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 189727 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 116969 2 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 116969 2 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 109380 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 109380 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 157463 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 157463 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 208207 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 208207 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 208207 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 208207 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 189727 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 189727 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 16653 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 16653 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 8105 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 8105 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 8127 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 8127 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 123150 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 123150 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 163849 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 163849 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 101880 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 101880 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 156001 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 156001 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 86409 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 86409 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 127286 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 127286 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 149044 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 149044 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 193398 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 193398 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 146732 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 146732 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 64451 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 64451 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 92081 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 92081 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 103068 68 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 103068 68 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 16588 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 16588 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 208064 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 208064 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 138027 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 138027 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 39220 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 39220 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 64832 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 64832 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 129978 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 129978 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 131374 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 131374 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 166836 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 166836 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 167120 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 167120 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 167190 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 167190 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 156852 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 156852 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 158885 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 158885 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 36963 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 36963 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 118110 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 118110 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 185296 18 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 185296 18 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 137689 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 137689 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 66964 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 66964 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 119372 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 119372 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 203886 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 203886 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 185011 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 185011 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 169198 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 169198 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 138019 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 138019 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 116649 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 116649 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 116961 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 116961 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 190147 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 190147 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 8565 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 8565 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 157079 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 157079 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 67013 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 67013 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 121320 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 121320 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 116649 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 116649 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 66927 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 66927 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 23022 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 23022 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 83245 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 83245 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 86726 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 86726 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 62019 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 62019 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 16794 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 16794 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 137819 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 137819 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 145345 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 145345 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 21363 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 21363 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 156227 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 156227 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 137820 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 137820 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 63791 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 63791 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 85358 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 85358 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 64424 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 64424 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 8342 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 8342 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 26781 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 26781 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 97315 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 97315 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 187092 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 187092 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 208363 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 208363 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 125889 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 125889 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 16816 9 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 16816 9 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 15929 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 15929 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 27512 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 27512 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 66116 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 66116 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 164256 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 164256 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 112236 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 112236 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 112236 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 112236 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 49 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 49 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 49 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 49 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 121324 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 121324 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 137742 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 137742 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 180922 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 180922 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 181018 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 181018 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 77995 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 77995 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 123151 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 123151 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 85359 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 85359 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 83261 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 83261 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 139517 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 139517 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 156246 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 156246 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 123167 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 123167 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 67246 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 67246 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 62404 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 62404 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 182758 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 182758 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 87074 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 87074 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 100087 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 100087 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 62402 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 62402 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 170633 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 170633 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 166044 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 166044 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 171136 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 171136 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 125848 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 125848 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 66238 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 66238 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 188682 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 188682 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 137800 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 137800 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 109384 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 109384 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 83245 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 83245 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 180732 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 180732 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 207775 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 207775 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 62406 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 62406 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 124098 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 124098 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 208128 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 208128 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 114605 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 114605 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 107367 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 107367 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 142091 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 142091 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 62400 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 62400 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 187115 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 187115 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 98137 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 98137 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 208306 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 208306 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 208306 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 208306 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 159547 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 159547 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 86413 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 86413 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 136623 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 136623 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 83472 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 83472 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 97380 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 97380 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 109379 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 109379 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 211090 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 4173 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 4173 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 8190 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 8190 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 194865 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 194865 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 196025 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 196025 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 83246 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 83246 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 183312 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 183312 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 8073 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 8073 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 92326 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 92326 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 98493 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 98493 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 3435 5 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 3435 5 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 3435 5 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 163797 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 163797 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 8329 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 8329 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 98419 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 98419 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 1956 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 1956 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 1956 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 208282 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 208282 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 15852 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 15852 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 158149 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 158149 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 64991 6 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 64991 6 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 121321 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 121321 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 109382 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 109382 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 15875 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 15875 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 98138 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 98138 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 62405 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 62405 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 207918 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 207918 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 98278 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 98278 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 64456 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 64456 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 207545 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 207545 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 205105 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 205105 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 166431 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 166431 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 159115 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 159115 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 163899 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 163899 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 123156 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 123156 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 8168 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 8168 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 208340 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 208340 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 208294 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 208294 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 208294 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 208294 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 181220 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 181220 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 18560 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 18560 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 166675 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 166675 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 62026 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 62026 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 166368 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 166368 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 157079 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 157079 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 15898 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 15898 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 69182 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 69182 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 3438 5 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 3438 5 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 3438 5 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 86416 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 86416 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 207931 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 207931 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 17281 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 17281 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 60754 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 60754 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 157118 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 157118 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 64450 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 64450 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 156608 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 156608 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 110868 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 110868 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 8890 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 8890 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 16763 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 16763 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 67946 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 67946 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 157839 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 157839 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 207977 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 207977 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 87746 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 87746 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 185395 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 185395 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 15833 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 15833 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 30693 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 30693 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 86411 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 86411 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 67057 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 67057 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 15901 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 15901 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 29217 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 29217 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 19845 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 19845 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 3437 22 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 3437 22 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 3437 22 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 110869 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 110869 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 64452 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 64452 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 16783 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 16783 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 97041 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 97041 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 189494 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 189494 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 189559 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 189559 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 141076 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 141076 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 181998 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 181998 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 123146 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 123146 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 141078 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 141078 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 208295 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 208295 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 189494 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 189494 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 164490 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 164490 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 204461 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 204461 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 137951 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 137951 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 208138 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 208138 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 163860 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 163860 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 158975 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 158975 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 189559 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 189559 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 208214 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 208214 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 15958 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 15958 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 189559 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 189559 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 166557 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 166557 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 211091 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 6 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 6 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 6 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 6 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 6 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 6 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 87075 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 87075 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 189559 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 189559 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 180138 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 180138 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 89948 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 89948 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 123168 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 123168 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 123672 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 123672 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 149212 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 149212 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 107553 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 107553 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 113092 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 113092 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 204847 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 204847 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 156743 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 156743 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 165763 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 165763 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 193384 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 193384 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 192518 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 192518 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 164208 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 164208 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 18553 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 18553 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 156377 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 156377 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 15932 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 15932 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 136651 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 136651 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 121328 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 121328 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 121328 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 121328 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 136651 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 136651 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 15930 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 15930 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 205144 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 205144 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 83262 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 83262 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 83285 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 83285 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 15876 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 15876 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 15931 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 15931 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 123152 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 123152 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 163020 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 163020 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 92303 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 92303 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 15960 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 15960 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 15855 37 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 15855 37 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 8193 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 8193 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 175315 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 175315 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 175315 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 175315 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 87073 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 87073 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 186794 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 186794 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 164841 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 164841 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 64455 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 64455 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 107261 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 107261 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 107261 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 107261 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 15874 17 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 15874 17 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 186979 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 186979 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 142336 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 142336 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 207833 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 207833 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 125843 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 125843 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 80842 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 80842 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 122043 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 122043 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 705 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 705 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 705 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 208367 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 208367 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 208367 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 208367 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 64601 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 64601 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 123943 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 123943 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 166675 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 166675 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 167046 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 167046 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 167219 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 167219 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 157505 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 157505 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 8671 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 8671 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 4338 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 4338 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 4338 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 4338 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 88551 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 88551 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 98920 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 98920 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 87747 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 87747 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 15896 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 15896 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 21507 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 21507 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 138313 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 138313 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 205235 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 205235 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 116556 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 116556 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 98221 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 98221 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 118972 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 118972 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 185988 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 185988 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 1990 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 1990 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 1990 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 1990 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 1990 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 1990 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 17207 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 17207 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 137634 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 137634 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 158895 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 158895 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 163532 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 163532 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 67635 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 67635 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 166932 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 166932 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 139544 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 139544 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 16589 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 16589 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 17947 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 17947 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 28915 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 28915 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 28915 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 28915 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 56 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 56 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 56 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 3435 5 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 3435 5 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 3435 5 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 3435 5 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 3435 5 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 3435 5 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 175219 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 175219 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 189561 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 189561 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 151363 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 151363 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 3435 5 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 3435 5 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 3435 5 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 8167 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 8167 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 119689 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 119689 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 119689 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 119689 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 205621 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 205621 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 175219 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 175219 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 189561 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 189561 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 93189 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 93189 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 83333 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 83333 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 205512 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 205512 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 124225 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 124225 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 64447 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 64447 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 207578 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 207578 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 15830 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 15830 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 137767 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 137767 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 156996 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 156996 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 98546 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 98546 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 16574 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 16574 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 8297 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 8297 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 37729 24 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 37729 24 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 164082 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 164082 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 123153 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 123153 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 123154 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 123154 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 4358 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 4358 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 76701 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 76701 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 111521 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 111521 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 190229 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 190229 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 15935 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 15935 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 77242 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 77242 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 15849 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 15849 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 123144 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 123144 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 139458 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 139458 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 16416 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 16416 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 211089 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 101881 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 101881 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 29964 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 29964 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 182129 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 182129 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 18548 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 18548 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 138679 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 138679 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 123147 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 123147 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 109643 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 109643 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 136872 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 136872 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 121318 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 121318 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 166421 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 166421 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 167371 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 167371 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 158392 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 158392 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 136872 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 136872 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 98857 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 98857 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 87362 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 87362 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 8892 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 8892 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 8892 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 8892 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 153553 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 153553 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 123148 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 123148 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 207474 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 207474 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 15895 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 15895 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 78298 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 78298 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 109383 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 109383 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 137733 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 137733 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 109643 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 109643 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 189742 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 189742 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 15853 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 15853 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 123165 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 123165 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 189742 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 189742 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 158179 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 158179 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 208442 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 208442 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 203983 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 203983 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 190236 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 190236 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 16917 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 16917 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 208364 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 208364 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 150483 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 150483 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 186980 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 186980 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 114150 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 114150 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 180075 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 180075 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 4377 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 4377 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 41 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 41 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 41 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 16839 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 16839 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 191621 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 191621 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 60757 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 60757 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 83314 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 83314 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 98321 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 98321 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 4632 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 4632 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 62408 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 62408 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 49727 47 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 49727 47 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 119692 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 119692 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 119692 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 119692 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 83478 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 83478 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 173533 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 173533 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 207876 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 207876 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 169351 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 169351 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 15873 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 15873 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 181687 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 181687 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 122905 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 122905 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 126602 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 126602 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 136722 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 136722 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 207937 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 207937 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 183034 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 183034 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 183118 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 183118 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 196326 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 196326 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 207072 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 207072 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 123142 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 123142 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 62401 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 62401 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 125804 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 125804 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 109381 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 109381 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 64449 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 64449 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 76759 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 76759 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 121326 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 121326 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 156610 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 156610 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 157045 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 157045 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 83148 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 83148 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 164789 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 164789 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 87929 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 87929 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 92327 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 92327 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 76667 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 76667 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 157940 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 157940 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 41 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 41 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 41 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 85362 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 85362 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 84401 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 84401 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 123629 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 123629 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 29822 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 29822 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 167057 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 167057 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 66089 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 66089 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 164495 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 164495 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 166133 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 166133 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 3914 5 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 3914 5 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 3914 5 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 136604 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 136604 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 3914 5 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 3914 5 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 3914 5 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 136604 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 136604 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 23576 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 23576 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 21375 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 21375 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 116710 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 116710 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 168453 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 168453 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 16780 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 16780 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 195700 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 195700 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 85736 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 85736 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 102968 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 102968 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 64543 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 64543 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 113332 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 113332 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 117373 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 117373 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 158810 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 158810 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 181386 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 181386 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 2387 75 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 2387 75 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 2387 75 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 204430 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 204430 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 205051 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 205051 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 109385 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 109385 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 87541 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 87541 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 15854 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 15854 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 77588 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 77588 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 155998 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 155998 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 204900 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 204900 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 204968 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 204968 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 167032 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 167032 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 4178 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 4178 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 4178 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 4178 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 114463 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 114463 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 163294 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 163294 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 114463 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 114463 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 163294 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 163294 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 15928 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 15928 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 123161 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 123161 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 207832 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 207832 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 85174 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 85174 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 77079 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 77079 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 2170 21 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 112334 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 112334 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 118681 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 118681 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 114152 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 114152 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 137913 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 137913 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 81558 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 81558 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 159797 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 159797 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 182574 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 182574 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 208449 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 208449 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 83323 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 83323 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 207800 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 207800 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 26948 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 26948 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 166490 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 166490 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 166912 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 166912 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 157723 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 157723 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 207527 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 207527 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 98305 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 98305 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 151363 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 151363 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 124391 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 124391 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 205671 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 205671 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 78298 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 78298 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 191621 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 191621 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 15878 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 15878 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 110870 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 110870 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 110870 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 110870 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 142032 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 142032 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 110870 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 110870 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 144814 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 144814 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 15900 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 15900 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 207784 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 207784 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 138132 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 138132 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 121325 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 121325 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 211088 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 1465 72 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 1465 72 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 1465 72 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 1465 72 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 1465 72 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 140888 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 140888 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 139279 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 139279 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 137824 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 137824 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 137896 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 137896 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 64454 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 64454 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 15959 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 15959 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 16655 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 16655 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 93076 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 93076 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 208321 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 208321 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 4240 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 4240 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 3916 8 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 3916 8 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 3916 8 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 74125 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 74125 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 208147 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 208147 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 2387 75 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 2387 75 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 2387 75 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 189544 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 189544 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 195393 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 195393 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 157512 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 157512 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 16771 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 16771 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 104876 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 104876 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 195393 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 195393 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 107058 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 107058 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 77247 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 77247 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 77140 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 77140 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 15880 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 15880 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 111654 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 111654 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 146731 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 146731 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 19946 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 19946 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 207761 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 207761 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 106949 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 106949 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 15897 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 15897 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 3436 15 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 3436 15 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 3436 15 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 181835 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 181835 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 60761 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 60761 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 158623 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 158623 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 85173 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 85173 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 208296 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 208296 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 208296 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 208296 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 97171 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 97171 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 205530 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 205530 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 207880 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 207880 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 175518 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 175518 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 175518 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 175518 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 101500 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 101500 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 208309 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 208309 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 208309 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 208309 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 194741 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 194741 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 138692 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 138692 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 16501 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 16501 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 86418 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 86418 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 112554 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 112554 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 112554 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 112554 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 8072 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 8072 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 85483 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 85483 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 159763 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 159763 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 179394 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 179394 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 8298 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 8298 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 64336 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 64336 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 123132 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 123132 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 17255 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 17255 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 60764 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 60764 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 136623 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 136623 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 136814 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 136814 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 166791 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 166791 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 8665 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 8665 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 15899 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 15899 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 934 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 934 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 934 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 186067 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 186067 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 136814 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 136814 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 85323 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 85323 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 138043 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 138043 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 188149 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 188149 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 16864 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 16864 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 137738 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 137738 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 156413 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 156413 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 156413 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 1845 5 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 1845 5 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 1845 5 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 60762 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 60762 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 166140 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 166140 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 62403 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 62403 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 205234 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 205234 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 205444 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 205444 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 11330 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 11330 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 11330 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 82890 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 82890 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 60760 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 60760 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 149215 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 149215 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 204850 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 204850 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 204997 4 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 204997 4 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 166675 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 166675 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 1849 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 1849 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 14421 57 35S-GTPGammaS - 1 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 330 9 0 8 2.1 CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC None
CHEMBL1200468 14421 57 35S-GTPGammaS - 1 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 330 9 0 8 2.1 CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC None
1357 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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
198 313 126 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 313 126 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
99 313 126 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 313 126 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 313 126 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 72 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 141 121 125I-Iodomelatonin -14791 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 125I-Iodomelatonin -14791 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 125I-Iodomelatonin -14791 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
4209 3163 75 125I-Mel -63095 33 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 3163 75 125I-Mel -63095 33 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 3163 75 125I-Mel -63095 33 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 3163 75 125I-Mel -63095 33 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 3163 75 125I-Mel -63095 33 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 3163 75 125I-Mel -63095 33 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2387 75 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 2387 75 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 2387 75 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 113343 79 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 113343 79 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 1849 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 1849 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 216102 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 112901 89 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 112901 89 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 2387 75 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 2387 75 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 2387 75 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 41 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 41 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 41 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 216099 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 216099 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 1465 72 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 1465 72 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 1465 72 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 1465 72 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 1465 72 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 216103 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 2387 75 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 2387 75 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 2387 75 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 112901 89 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 112901 89 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 113343 79 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 113343 79 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 3756 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 3756 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 3756 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 3756 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 3756 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 216099 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
198 313 126 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
198 313 126 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 313 126 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 313 126 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
99 313 126 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
99 313 126 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 313 126 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 313 126 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 313 126 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 313 126 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 1532 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 1532 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 1532 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 1416 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 1416 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 1416 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 3288 99 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 1986 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 1986 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 2387 75 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 3915 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 3915 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 3914 5 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 3914 5 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 3914 5 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 3914 5 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 3914 5 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 3914 5 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 47 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 216 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 216 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 216 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 56 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 56 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 56 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 56 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 56 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 56 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 56 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 56 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 56 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 56 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 56 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 56 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 3917 13 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 3917 13 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 3917 13 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 3911 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 3911 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 3911 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 814 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 814 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 814 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 2485 139 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 3756 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 3756 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 3756 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 3756 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 3756 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 14421 57 None - 1 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 330 9 0 8 2.1 CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC None
CHEMBL1200468 14421 57 None - 1 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 330 9 0 8 2.1 CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC None
1351 2395 21 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 2395 21 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 2395 21 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 3433 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 3433 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 3433 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 41 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 41 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 41 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 41 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 41 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 41 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 41 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 41 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 41 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 1845 5 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 1845 5 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 1845 5 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 1845 5 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 1845 5 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 1845 5 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 3436 15 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 3436 15 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 3436 15 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 2170 21 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 2170 21 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 2170 21 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 3435 5 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 3435 5 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 3435 5 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 3434 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 3434 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 1990 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 1990 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 1990 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 3437 22 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 3437 22 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 3437 22 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 3438 5 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 3438 5 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 3438 5 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 1849 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 1849 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 1849 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 1849 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