Ligand source activities (1 row/activity)





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DOI

57781216 132625 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 132625 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 8314 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 8314 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 8314 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 191610 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 191610 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 191376 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 191376 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 191637 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 191637 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 192108 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 192108 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 191783 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 191783 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 193046 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 193046 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 173446 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 173446 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 192075 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 192075 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 191610 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 191610 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 193112 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 193112 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 106892 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 106892 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 191376 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 191376 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 7101 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 7101 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 7101 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 7101 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 7101 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 173254 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 173254 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 173530 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 173530 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 191783 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 191783 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 191790 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 191790 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 192618 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 192618 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 192075 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 192075 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 197008 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 197008 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 191637 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 191637 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 192108 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 192108 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 193046 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 193046 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 199297 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 199297 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 68793 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 68793 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 199297 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 199297 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 73701 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 73701 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 196926 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 196926 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 192723 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 192723 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 166299 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 166299 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 173269 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 173269 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 174060 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 174060 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 129941 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 129941 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 191226 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 191226 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 192921 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 192921 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 144462 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 144462 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 144598 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 144598 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 196926 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 196926 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 129940 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 129940 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 191790 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 191790 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 15662 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 15662 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 173454 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 173454 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 173998 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 173998 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 166454 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 166454 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 173570 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 173570 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 173691 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 173691 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 163156 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 163156 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 15615 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 15615 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 129926 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 129926 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 35688 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 35688 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 15415 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 15415 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 67526 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 67526 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 119013 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 119013 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 197008 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 197008 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 173836 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 173836 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 67538 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 67538 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 15640 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 15640 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 93849 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 93849 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 129925 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 129925 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 163631 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 163631 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 49994 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 49994 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 10681 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 10681 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 10681 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 69182 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 69182 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 164723 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 164723 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 163897 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 163897 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 129932 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 129932 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 173276 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 173276 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 129943 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 129943 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 67529 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 67529 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 191226 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 191226 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 15293 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 15293 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 15443 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 15443 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 15661 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 15661 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 15416 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 15416 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 93850 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 93850 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 173811 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 173811 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 173899 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 173899 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 163025 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 163025 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 69175 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 69175 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 128098 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 128098 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 119099 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 119099 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 15417 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 15417 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 197749 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 197749 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 15438 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 15438 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 69174 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 69174 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 129921 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 129921 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 129923 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 129923 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 214756 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 214756 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 165674 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 165674 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 6928 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 6928 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 6928 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 6928 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 111996 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 111996 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 7601 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 7601 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 7601 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 187511 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 187511 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 7101 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 7101 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 7101 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 7101 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 7101 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 129924 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 129924 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 128095 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 128095 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 144516 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 144516 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 173336 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 173336 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 68802 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 68802 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 15437 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 15437 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 192174 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 192174 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 174150 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 174150 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 164284 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 164284 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 129931 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 129931 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 67537 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 67537 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 186854 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 186854 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 128106 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 128106 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 129930 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 129930 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 10208 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 10208 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 10208 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 128096 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 128096 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 164242 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 164242 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 129927 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 129927 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 173390 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 173390 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 67527 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 67527 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 7721 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 7721 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 7721 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 144597 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 144597 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 144412 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 144412 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 7492 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 7492 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 7492 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 189537 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 189537 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 187701 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 187701 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 15337 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 15337 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 165852 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 165852 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 119111 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 119111 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 173336 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 173336 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 173708 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 173708 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 174015 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 174015 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 67528 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 67528 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 144578 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 144578 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 128097 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 128097 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 173402 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 173402 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 129944 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 129944 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 164291 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 164291 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 186917 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 186917 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 144467 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 144467 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 15487 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 15487 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 173210 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 173210 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 128101 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 128101 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 36673 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 36673 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 10211 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 10211 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 10211 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 144627 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 144627 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 164958 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 164958 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 173454 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 173454 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 144509 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 144509 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 93848 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 93848 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 129945 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 129945 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 173969 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 173969 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 93846 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 93846 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 15488 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 15488 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 144511 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 144511 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 162865 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 162865 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 165664 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 165664 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 129920 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 129920 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 80921 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 80921 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 67536 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 67536 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 128103 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 128103 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 128099 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 128099 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 202479 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 202479 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 117644 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 117644 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 7004 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 7004 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 7004 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 67527 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 67527 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 10686 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 10686 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 10686 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 10691 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 10691 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 10692 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 10692 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 10690 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 10690 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 7342 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 7342 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 7342 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 7342 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 9458 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 9458 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 9458 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 128106 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 128106 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 37739 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 37739 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 119099 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 119099 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 132630 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 132630 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 132628 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 132628 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 132632 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 132632 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 132625 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 132625 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 132622 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 132622 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 167615 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 167615 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 132638 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 132638 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 132627 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 132627 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 132624 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 132624 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 132631 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 132631 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 16546 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 16546 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 168346 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 168346 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 167743 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 167743 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 132637 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 132637 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 167612 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 167612 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 105005 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 105005 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 123565 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 123565 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 167609 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 167609 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 132634 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 132634 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 132636 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 132636 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 116600 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 116600 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 132635 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 132635 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 35576 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 35576 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 35715 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 35715 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 116468 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 116468 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 181802 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 181802 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 132623 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 132623 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 6858 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 6858 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 6858 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 6858 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 36093 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 36093 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 148740 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 148740 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 15022 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 15022 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 16519 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 16519 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 16614 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 16614 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 169530 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 169530 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 116600 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 116600 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 14809 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 14809 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 36624 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 36624 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 145438 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 145438 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 16496 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 16496 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 36060 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 36060 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 125518 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 125518 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 195493 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 195493 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 16175 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 16175 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 35522 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 35522 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 125934 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 125934 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 195493 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 195493 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 36168 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 36168 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 125648 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 125648 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 171827 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 171827 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 35690 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 35690 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 36076 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 36076 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 36265 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 36265 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 36310 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 36310 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 37023 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 37023 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 37407 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 37407 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 38479 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 38479 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 126029 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 126029 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 106978 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 106978 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 125999 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 125999 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 132629 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 132629 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 76603 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 76603 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 37181 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 37181 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 37488 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 37488 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 123311 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 123311 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 125784 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 125784 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 126207 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 126207 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 199886 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 199886 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 35664 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 35664 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 35688 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 35688 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 38823 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 38823 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 126156 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 126156 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 172035 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 172035 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 33635 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 33635 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 36452 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 36452 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 132626 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 132626 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 16638 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 16638 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 35704 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 35704 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 35762 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 35762 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 35784 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 35784 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 35963 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 35963 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 168450 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 168450 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 76268 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 76268 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 33481 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 33481 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 34190 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 34190 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 177215 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 177215 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 36635 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 36635 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 39975 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 39975 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 125921 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 125921 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 126178 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 126178 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 175234 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 175234 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 35937 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 35937 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 36941 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 36941 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 39572 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 39572 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 74032 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 74032 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 16863 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 16863 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 195565 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 195565 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 132633 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 132633 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 35665 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 35665 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 36298 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 36298 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 36673 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 36673 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 36675 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 36675 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 36832 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 36832 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 126222 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 126222 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 34191 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 34191 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 36130 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 36130 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 39676 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 39676 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 126793 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 126793 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 117643 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 117643 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 36687 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 36687 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 145017 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 145017 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 105795 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 105795 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 73780 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 73780 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 16191 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 16191 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 36946 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 36946 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 38372 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 38372 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 37416 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 37416 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 126104 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 126104 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 143122 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 143122 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 111996 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 111996 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 182375 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 182375 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 194151 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 194151 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 38481 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 38481 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 39181 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 39181 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 175385 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 175385 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 115981 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 115981 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 122268 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 122268 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 123534 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 123534 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 176098 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 176098 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 182274 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 182274 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 37483 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 37483 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 38170 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 38170 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 16570 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 16570 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 37076 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 37076 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 126205 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 126205 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 194338 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 194338 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 15209 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 15209 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 36386 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 36386 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 37565 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 37565 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 38378 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 38378 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 123572 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 123572 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 125525 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 125525 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 106857 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 106857 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 78480 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 78480 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 182478 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 182478 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 16076 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 16076 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 35613 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 35613 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 36230 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 36230 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 36609 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 36609 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 115342 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 115342 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 36721 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 36721 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 125576 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 125576 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 125820 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 125820 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 126061 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 126061 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 126151 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 126151 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 66853 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 66853 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 36279 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 36279 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 36513 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 36513 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 36849 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 36849 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 38911 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 38911 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 39993 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 39993 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 73672 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 73672 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 194149 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 194149 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 199434 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 199434 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 16205 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 16205 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 36938 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 36938 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 37399 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 37399 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 132585 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 132585 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 35940 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 35940 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 125924 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 125924 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 38549 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 38549 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 39292 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 39292 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 123566 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 123566 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 38833 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 38833 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 39870 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 39870 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 174998 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 174998 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 36355 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 36355 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 123180 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 123180 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 125755 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 125755 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 125821 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 125821 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 126121 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 126121 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 181763 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 181763 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 36839 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 36839 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 38482 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 38482 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 39662 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 39662 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 125556 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 125556 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 37653 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 37653 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 126118 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 126118 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 37018 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 37018 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 194474 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 194474 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 68179 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 68179 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9458 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 9458 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 9458 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 29565 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 29565 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 106892 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 106892 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 119357 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 119357 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 106892 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 106892 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 123214 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 123214 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 68789 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 68789 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 6858 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 6858 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 6858 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 6858 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 10061 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 10061 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 10061 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 10061 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 10061 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 10061 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 10061 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 10061 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 10061 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 10061 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 123353 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 123353 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 124931 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 124931 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 113655 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 113655 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 68788 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 68788 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 30335 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 30335 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 70571 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 70571 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 192674 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 192674 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 42613 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 42613 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 26617 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 26617 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 129940 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 129940 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 6866 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 6866 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 6866 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 132625 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 132625 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 68791 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 68791 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 132631 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 132631 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 70569 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 70569 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 214344 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 214344 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 71763 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 71763 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 144853 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 144853 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 93189 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 93189 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 70570 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 70570 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 68787 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 68787 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 39486 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 39486 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 104932 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 104932 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 212397 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 212397 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 74374 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 74374 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 85564 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 85564 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 85569 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 85569 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 85573 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 85573 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 85574 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 85574 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 85575 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 85575 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 85579 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 85579 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 8198 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 8198 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 8198 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 8198 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 8198 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 8198 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 26257 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 26257 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 68799 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 68799 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 93187 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 93187 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 8314 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 8314 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 8314 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 132624 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 132624 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 132627 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 132627 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 6858 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 6858 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 6858 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 6858 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 68797 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 68797 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 123432 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 123432 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 15416 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 15416 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 9174 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 9174 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 9174 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 37734 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 37734 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 6858 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 6858 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 6858 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 6858 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 108568 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 108568 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 70566 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 70566 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 70568 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 70568 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 15293 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 15293 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 107386 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 107386 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 107386 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 107386 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 27028 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 27028 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 29024 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 29024 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 7101 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 7101 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 7101 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 7101 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 7101 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 173254 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 173254 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 93190 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 93190 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 28135 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 28135 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 68790 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 68790 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 26967 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 26967 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7101 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 7101 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 7101 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 7101 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 7101 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7101 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 7101 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 7101 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 7101 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 7101 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7101 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 7101 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 7101 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 7101 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 7101 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 74097 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 74097 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 33850 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 33850 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 116600 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 116600 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 178571 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 178571 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 116600 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 116600 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 116600 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 116600 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 70567 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 70567 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 193094 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 193094 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 126064 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 126064 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 7101 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 7101 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 7101 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 7101 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 7101 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 105689 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 105689 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 26256 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 26256 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 27476 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 27476 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 174658 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 174658 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 67526 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 67526 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 193051 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 193051 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 144689 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 144689 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 144838 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 144838 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 93192 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 93192 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 123406 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 123406 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 105378 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 105378 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 132634 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 132634 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 67526 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 67526 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 67526 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 67526 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 15487 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 15487 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 173276 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 173276 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 174060 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 174060 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 166299 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 166299 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 192698 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 192698 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 93185 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 93185 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 200636 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 200636 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 70573 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 70573 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 191637 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 191637 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 74300 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 74300 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 192955 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 192955 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 26617 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 26617 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 175103 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 175103 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 15417 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 15417 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 193112 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 193112 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 212285 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 212285 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 132635 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 132635 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 173336 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 173336 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 173446 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 173446 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 26607 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 26607 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 192108 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 192108 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 28135 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 28135 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 132623 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 132623 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 132636 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 132636 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 70572 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 70572 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 10210 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 10210 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 10210 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 10210 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 10210 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 10210 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 10210 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 10210 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 10210 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7601 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 7601 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 7601 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 10211 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 10211 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 10211 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 10211 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 10211 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 10211 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 74101 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 74101 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 10211 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 10211 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 10211 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 173336 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 173336 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 173801 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 173801 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 174015 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 174015 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 10211 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 10211 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 10211 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 164723 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 164723 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 193046 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 193046 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 121589 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 121589 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 121589 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 121589 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 15615 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 15615 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 33891 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 33891 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 28254 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 28254 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 25321 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 25321 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 129941 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 129941 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 192723 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 192723 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 22651 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 22651 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 214405 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 214405 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 119648 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 119648 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 10683 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 10683 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 10683 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 123589 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 123589 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 15415 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 15415 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 123371 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 123371 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 173390 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 173390 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 173708 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 173708 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 162865 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 162865 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 10689 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 10689 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 10689 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 95328 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 95328 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 191610 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 191610 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 68794 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 68794 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 35726 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 35726 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 15640 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 15640 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 22649 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 22649 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 75451 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 75451 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 27447 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 27447 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 74791 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 74791 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 69776 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 69776 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 129119 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 129119 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 130053 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 130053 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 136948 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 136948 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 211959 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 211959 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 192618 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 192618 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 173402 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 173402 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 173530 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 173530 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 214568 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 214568 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 15639 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 15639 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 125269 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 125269 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 15488 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 15488 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 103772 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 103772 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 191376 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 191376 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 192921 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 192921 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 68792 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 68792 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 68798 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 68798 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 202003 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 202003 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 83477 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 83477 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 7004 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 7004 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 7004 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 37425 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 37425 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 26758 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 26758 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 117645 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 117645 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 191783 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 191783 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 143626 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 143626 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 191342 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 191342 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 85073 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 85073 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 143626 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 143626 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 197008 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 197008 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 119099 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 119099 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 119099 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 119099 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 119099 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 119099 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 74267 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 74267 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 123863 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 123863 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 175326 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 175326 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 123692 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 123692 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 77084 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 77084 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 67529 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 67529 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 192400 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 192400 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 68804 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 68804 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 31509 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 31509 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 122135 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 122135 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 117642 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 117642 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 74269 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 74269 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 165852 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 165852 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 15661 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 15661 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 67527 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 67527 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 74269 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 74269 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 68803 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 68803 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 181001 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 181001 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 123318 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 123318 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 15438 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 15438 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 163858 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 163858 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 129944 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 129944 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 144676 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 144676 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 84860 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 84860 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 22622 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 22622 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 157002 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 157002 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 202266 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 202266 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 214856 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 214856 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 199297 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 199297 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 123370 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 123370 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 144462 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 144462 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 166454 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 166454 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 27373 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 27373 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 144470 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 144470 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 131185 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 131185 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 94138 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 94138 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 83889 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 83889 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 212004 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 212004 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 36673 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 36673 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 212073 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 212073 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 156023 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 156023 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 181456 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 181456 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 203050 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 203050 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 181456 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 181456 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 6857 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 6857 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 6857 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 6912 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 6912 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 6912 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 67530 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 67530 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 22603 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 22603 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 73063 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 73063 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 212151 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 212151 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 108588 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 108588 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 181703 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 181703 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 181703 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 181703 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 203342 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 203342 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 22623 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 22623 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 72919 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 72919 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 28552 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 28552 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 84092 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 84092 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 143467 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 143467 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 203524 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 203524 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 75850 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 75850 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 71764 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 71764 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 203342 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 203342 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 10210 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 10210 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 10210 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 130457 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 130457 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 116163 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 116163 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 10210 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 10210 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 10210 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 6857 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 6857 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 6857 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 98984 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 98984 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 188222 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 188222 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 22628 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 22628 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 22706 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 22706 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 214962 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 214962 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 129923 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 129923 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 23294 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 23294 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 83899 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 83899 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 214889 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 214889 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 14477 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 14477 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 23546 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 23546 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 211641 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 211641 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 143467 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 143467 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 170997 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 170997 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 214623 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 214623 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 144766 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 144766 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 196403 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 196403 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 22666 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 22666 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 215116 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 215116 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 90047 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 90047 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 22699 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 22699 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 22705 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 22705 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 196403 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 196403 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 93846 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 93846 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 67533 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 67533 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 129933 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 129933 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 215154 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 215154 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 215154 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 215154 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 165901 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 165901 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 188909 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 188909 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 197408 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 197408 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 96660 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 96660 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 94523 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 94523 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 188610 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 188610 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 15027 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 15027 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 10685 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 10685 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 10685 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 214883 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 214883 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 201546 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 201546 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 95329 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 95329 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 10685 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 10685 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 10685 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 94140 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 94140 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 123191 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 123191 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 10685 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 10685 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 10685 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 10685 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 10685 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 10685 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 191226 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 191226 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 129921 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 129921 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 130720 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 130720 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 68802 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 68802 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 23660 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 23660 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 103319 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 103319 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 96255 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 96255 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 129927 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 129927 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 181990 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 181990 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 215086 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 215086 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 215086 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 215086 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 93846 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 93846 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 93846 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 93846 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 193893 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 193893 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 22604 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 22604 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 188612 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 188612 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 128095 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 128095 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 94139 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 94139 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 119329 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 119329 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 71227 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 71227 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 214598 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 214598 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 108324 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 108324 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 144587 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 144587 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 177656 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 177656 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 125983 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 125983 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 125983 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 125983 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 177656 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 177656 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 23278 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 23278 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 15191 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 15191 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 195762 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 195762 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 196926 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 196926 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 186666 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 186666 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 104942 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 104942 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 195762 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 195762 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 146229 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 146229 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 202875 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 202875 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 94307 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 94307 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 189110 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 189110 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 173036 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 173036 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 175895 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 175895 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 144627 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 144627 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 144509 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 144509 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 9166 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 9166 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 9166 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 67537 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 67537 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 166111 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 166111 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 73099 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 73099 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 129488 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 129488 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 171392 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 171392 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 6925 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 6925 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 6925 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 95327 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 95327 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 73825 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 73825 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 115277 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 115277 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 115277 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 115277 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 23610 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 23610 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 10681 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 10681 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 10681 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 128097 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 128097 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 144510 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 144510 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 194929 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 194929 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 34289 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 34289 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 128101 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 128101 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 147838 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 147838 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 129942 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 129942 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 11448 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 11448 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 84769 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 84769 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 196506 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 196506 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 211809 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 211809 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 105089 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 105089 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 211762 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 211762 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 196506 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 196506 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 196506 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 196506 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 196506 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 196506 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 123747 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 123747 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 116157 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 116157 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 164242 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 164242 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 214986 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 214986 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 214986 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 214986 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 196506 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 196506 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 23425 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 23425 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 14877 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 14877 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 14899 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 14899 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 129928 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 129928 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 170628 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 170628 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 108657 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 108657 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 162780 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 162780 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 93184 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 93184 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 134064 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 134064 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 155823 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 155823 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 200177 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 200177 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 153510 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 153510 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 71225 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 71225 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 98856 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 98856 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 109845 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 109845 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 23360 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 23360 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 214843 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 214843 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 144805 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 144805 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 45994 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 45994 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 71606 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 71606 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 136756 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 136756 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 138152 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 138152 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 173615 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 173615 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 173899 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 173899 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 173969 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 173969 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 163631 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 163631 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 165664 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 165664 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 43737 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 43737 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 124888 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 124888 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 192075 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 192075 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 144467 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 144467 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 73738 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 73738 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 126150 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 126150 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 210665 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 210665 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 191790 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 191790 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 175977 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 175977 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 144797 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 144797 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 123427 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 123427 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 123739 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 123739 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 196926 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 196926 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 15337 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 15337 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 163858 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 163858 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 73787 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 73787 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 128098 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 128098 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 123427 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 123427 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 73701 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 73701 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 29794 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 29794 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 90020 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 90020 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 93501 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 93501 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 68793 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 68793 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 23566 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 23566 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 144597 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 144597 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 152123 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 152123 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 28135 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 28135 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 163006 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 163006 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 144598 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 144598 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 70565 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 70565 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 92133 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 92133 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 71198 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 71198 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 15114 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 15114 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 33554 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 33554 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 104090 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 104090 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 193871 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 193871 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 215142 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 215142 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 132667 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 132667 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 23588 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 23588 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 22701 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 22701 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 34285 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 34285 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 72890 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 72890 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 171035 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 171035 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 119013 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 119013 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 119013 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 119013 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 6928 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 6928 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 6928 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 6928 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 128102 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 128102 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 144520 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 144520 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 187701 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 187701 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 187797 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 187797 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 84770 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 84770 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 129929 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 129929 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 92134 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 92134 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 90036 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 90036 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 146295 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 146295 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 163025 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 163025 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 129945 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 129945 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 74020 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 74020 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 69178 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 69178 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 189537 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 189537 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 93849 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 93849 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 106863 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 106863 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 69176 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 69176 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 177412 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 177412 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 172823 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 172823 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 177915 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 177915 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 132626 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 132626 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 73012 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 73012 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 195461 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 195461 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 144578 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 144578 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 116161 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 116161 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 90020 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 90020 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 187511 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 187511 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 214554 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 214554 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 69180 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 69180 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 130876 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 130876 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 214907 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 214907 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 121383 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 121383 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 114144 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 114144 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 148869 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 148869 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 69174 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 69174 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 193894 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 193894 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 104913 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 104913 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 215085 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 215085 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 215085 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 215085 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 166326 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 166326 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 93188 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 93188 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 143401 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 143401 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 90247 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 90247 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 104155 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 104155 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 116156 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 116156 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 217869 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 10945 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 10945 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 14962 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 14962 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 201644 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 201644 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 202804 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 202804 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 90021 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 90021 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 190091 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 190091 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 14845 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 14845 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 99101 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 99101 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 105269 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 105269 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 10208 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 10208 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 10208 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 170576 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 170576 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 15101 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 15101 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 105195 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 105195 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 8737 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 8737 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 8737 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 215061 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 215061 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 22624 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 22624 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 164928 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 164928 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 71765 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 71765 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 128099 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 128099 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 116159 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 116159 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 22647 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 22647 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 104914 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 104914 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 69179 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 69179 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 214697 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 214697 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 105054 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 105054 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 71230 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 71230 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 214324 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 214324 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 211884 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 211884 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 173210 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 173210 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 165894 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 165894 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 170678 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 170678 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 129934 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 129934 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 14940 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 14940 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 215119 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 215119 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 215073 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 215073 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 215073 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 215073 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 187999 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 187999 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 25332 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 25332 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 173454 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 173454 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 68800 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 68800 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 173147 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 173147 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 163858 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 163858 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 22670 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 22670 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 75957 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 75957 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 10211 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 10211 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 10211 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 93191 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 93191 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 214710 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 214710 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 24053 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 24053 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 67528 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 67528 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 163897 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 163897 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 71224 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 71224 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 163387 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 163387 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 117645 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 117645 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 15662 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 15662 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 23535 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 23535 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 74721 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 74721 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 164618 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 164618 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 214756 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 214756 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 94521 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 94521 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 192174 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 192174 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 22605 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 22605 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 37466 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 37466 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 93186 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 93186 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 73831 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 73831 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 22673 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 22673 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 35990 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 35990 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 26617 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 26617 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 10210 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 10210 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 10210 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 117646 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 117646 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 71226 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 71226 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 23555 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 23555 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 103816 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 103816 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 196273 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 196273 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 196338 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 196338 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 147854 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 147854 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 188777 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 188777 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 129924 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 129924 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 147856 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 147856 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 215074 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 215074 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 196273 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 196273 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 171269 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 171269 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 211240 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 211240 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 144729 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 144729 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 214917 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 214917 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 170639 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 170639 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 165754 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 165754 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 196338 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 196338 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 214993 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 214993 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 22730 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 22730 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 196338 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 196338 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 173336 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 173336 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 217870 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 6930 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 6930 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 6930 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 6930 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 6930 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 6930 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 93850 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 93850 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 196338 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 196338 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 186917 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 186917 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 96723 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 96723 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 129946 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 129946 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 130450 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 130450 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 155991 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 155991 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 114330 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 114330 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 119869 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 119869 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 211626 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 211626 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 163522 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 163522 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 172542 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 172542 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 200163 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 200163 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 199297 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 199297 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 170987 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 170987 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 25325 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 25325 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 163156 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 163156 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 22704 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 22704 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 143429 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 143429 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 128106 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 128106 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 128106 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 128106 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 143429 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 143429 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 22702 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 22702 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 211923 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 211923 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 90037 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 90037 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 90060 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 90060 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 22648 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 22648 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 22703 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 22703 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 129930 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 129930 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 169799 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 169799 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 99078 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 99078 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 22732 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 22732 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 22627 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 22627 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 14965 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 14965 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 182094 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 182094 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 182094 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 182094 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 93848 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 93848 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 193573 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 193573 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 171620 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 171620 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 71229 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 71229 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 114038 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 114038 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 114038 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 114038 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 22646 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 22646 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 193758 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 193758 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 149114 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 149114 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 214612 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 214612 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 132621 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 132621 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 87617 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 87617 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 128821 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 128821 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 7492 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 7492 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 7492 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 215146 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 215146 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 215146 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 215146 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 71375 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 71375 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 130721 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 130721 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 173454 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 173454 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 173825 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 173825 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 173998 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 173998 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 164284 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 164284 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 15443 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 15443 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 11110 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 11110 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 11110 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 11110 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 95326 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 95326 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 105696 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 105696 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 94522 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 94522 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 22668 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 22668 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 28279 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 28279 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 145091 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 145091 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 212014 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 212014 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 123334 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 123334 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 104997 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 104997 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 125750 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 125750 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 192767 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 192767 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 8771 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 8771 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 8771 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 8771 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 8771 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 8771 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 23979 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 23979 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 144412 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 144412 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 165674 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 165674 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 170311 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 170311 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 74409 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 74409 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 173711 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 173711 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 146322 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 146322 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 23361 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 23361 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 24719 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 24719 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 35688 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 35688 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 35688 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 35688 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 6950 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 6950 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 6950 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 10208 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 10208 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 10208 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 10208 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 10208 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 10208 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 181998 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 181998 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 196340 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 196340 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 158142 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 158142 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 10208 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 10208 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 10208 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 14939 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 14939 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 126467 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 126467 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 126467 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 126467 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 212400 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 212400 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 181998 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 181998 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 196340 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 196340 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 99964 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 99964 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 90108 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 90108 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 212291 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 212291 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 131003 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 131003 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 71221 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 71221 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 214357 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 214357 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 22602 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 22602 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 144545 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 144545 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 163775 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 163775 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 105322 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 105322 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 23346 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 23346 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 15069 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 15069 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 44503 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 44503 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 170861 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 170861 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 129931 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 129931 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 129932 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 129932 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 11130 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 11130 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 83476 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 83476 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 118298 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 118298 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 197008 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 197008 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 22707 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 22707 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 84017 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 84017 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 22621 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 22621 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 129922 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 129922 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 146236 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 146236 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 23188 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 23188 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 217868 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 108658 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 108658 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 36737 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 36737 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 188908 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 188908 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 25320 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 25320 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 145457 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 145457 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 129925 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 129925 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 116420 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 116420 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 143650 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 143650 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 128096 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 128096 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 173200 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 173200 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 174150 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 174150 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 165171 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 165171 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 143650 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 143650 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 105633 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 105633 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 94137 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 94137 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 15664 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 15664 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 15664 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 15664 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 160332 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 160332 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 129926 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 129926 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 214253 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 214253 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 22667 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 22667 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 85073 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 85073 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 116160 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 116160 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 144511 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 144511 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 116420 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 116420 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 196521 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 196521 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 22625 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 22625 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 129943 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 129943 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 196521 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 196521 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 164958 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 164958 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 215221 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 215221 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 210762 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 210762 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 197015 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 197015 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 23689 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 23689 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 215143 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 215143 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 157262 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 157262 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 193759 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 193759 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 120927 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 120927 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 186854 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 186854 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 11149 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 11149 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 6912 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 6912 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 6912 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 23611 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 23611 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 198400 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 198400 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 67531 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 67531 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 90089 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 90089 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 105097 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 105097 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 11404 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 11404 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 69182 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 69182 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 56501 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 56501 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 126470 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 126470 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 126470 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 126470 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 90253 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 90253 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 180312 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 180312 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 214655 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 214655 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 176130 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 176130 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 22645 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 22645 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 188466 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 188466 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 129683 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 129683 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 133380 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 133380 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 143500 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 143500 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 214716 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 214716 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 189813 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 189813 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 189897 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 189897 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 203105 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 203105 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 213851 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 213851 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 129920 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 129920 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 69175 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 69175 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 132582 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 132582 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 116158 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 116158 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 71223 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 71223 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 83534 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 83534 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 128104 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 128104 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 163389 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 163389 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 163824 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 163824 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 89923 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 89923 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 171568 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 171568 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 94704 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 94704 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 99102 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 99102 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 83442 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 83442 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 164719 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 164719 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 6912 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 6912 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 6912 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 92137 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 92137 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 91176 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 91176 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 130407 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 130407 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 36595 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 36595 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 173836 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 173836 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 72863 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 72863 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 171274 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 171274 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 172912 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 172912 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 10686 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 10686 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 10686 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 143382 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 143382 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 10686 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 10686 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 10686 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 143382 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 143382 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 30348 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 30348 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 28147 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 28147 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 123488 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 123488 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 175232 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 175232 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 23552 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 23552 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 202479 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 202479 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 92511 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 92511 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 109745 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 109745 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 71317 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 71317 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 120109 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 120109 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 124151 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 124151 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 165589 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 165589 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 188165 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 188165 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 9166 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 9166 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 9166 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 211209 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 211209 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 211830 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 211830 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 116162 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 116162 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 94316 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 94316 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 22626 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 22626 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 84363 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 84363 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 162777 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 162777 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 211679 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 211679 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 211747 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 211747 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 173811 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 173811 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 10950 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 10950 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 10950 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 10950 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 121241 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 121241 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 170073 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 170073 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 121241 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 121241 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 170073 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 170073 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 22700 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 22700 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 129939 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 129939 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 214611 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 214611 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 91949 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 91949 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 83854 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 83854 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 8951 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 8951 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 8951 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 8951 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 8951 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 8951 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 8951 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 8951 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 8951 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 8951 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 8951 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 8951 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 119111 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 119111 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 125459 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 125459 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 120929 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 120929 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 144691 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 144691 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 88333 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 88333 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 166576 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 166576 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 189353 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 189353 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 215228 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 215228 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 90098 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 90098 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 214579 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 214579 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 33721 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 33721 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 173269 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 173269 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 173691 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 173691 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 164502 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 164502 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 214306 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 214306 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 105081 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 105081 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 158142 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 158142 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 131169 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 131169 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 212450 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 212450 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 85073 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 85073 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 198400 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 198400 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 22650 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 22650 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 117647 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 117647 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 117647 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 117647 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 148810 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 148810 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 117647 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 117647 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 151592 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 151592 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 22672 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 22672 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 214563 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 214563 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 144910 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 144910 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 128103 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 128103 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 217867 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 8247 72 None -38 38 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 8247 72 None -38 38 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 8247 72 None -38 38 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 8247 72 None -38 38 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 8247 72 None -38 38 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 147666 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 147666 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 146057 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 146057 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 144602 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 144602 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 144674 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 144674 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 71228 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 71228 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 22731 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 22731 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 23427 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 23427 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 99851 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 99851 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 215100 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 215100 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 11012 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 11012 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 10688 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 10688 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 10688 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 80900 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 80900 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 214926 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 214926 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 9166 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 9166 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 9166 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 196323 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 196323 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 202172 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 202172 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 164291 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 164291 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 23543 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 23543 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 111653 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 111653 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 202172 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 202172 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 113835 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 113835 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 84022 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 84022 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 83915 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 83915 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 22652 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 22652 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 118431 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 118431 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 153509 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 153509 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 26718 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 26718 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 214540 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 214540 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 113726 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 113726 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 22669 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 22669 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 10209 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 10209 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 10209 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 188614 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 188614 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 67535 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 67535 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 165402 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 165402 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 91948 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 91948 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 215075 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 215075 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 215075 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 215075 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 103946 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 103946 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 212309 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 212309 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 214659 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 214659 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 182297 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 182297 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 182297 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 182297 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 108277 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 108277 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 215088 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 215088 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 215088 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 215088 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 201520 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 201520 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 145470 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 145470 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 23273 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 23273 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 93193 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 93193 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 119331 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 119331 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 119331 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 119331 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 14844 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 14844 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 92258 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 92258 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 166542 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 166542 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 186173 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 186173 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 15070 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 15070 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 71110 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 71110 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 129910 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 129910 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 24027 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 24027 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 67538 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 67538 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 143401 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 143401 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 143592 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 143592 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 173570 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 173570 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 15437 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 15437 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 22671 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 22671 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 7721 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 7721 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 7721 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 192846 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 192846 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 143592 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 143592 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 92098 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 92098 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 144821 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 144821 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 194928 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 194928 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 23636 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 23636 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 144516 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 144516 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 163192 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 163192 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 163192 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 8626 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 8626 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 8626 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 67536 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 67536 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 172919 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 172919 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 69177 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 69177 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 212013 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 212013 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 212223 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 212223 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 18102 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 18102 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 18102 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 89665 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 89665 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 67534 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 67534 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 155994 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 155994 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 211629 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 211629 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 211776 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 211776 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 173454 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 173454 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7101 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 7101 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 7101 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 7101 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 7101 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 8630 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 8630 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 21193 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 21193 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 7101 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 7101 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 7101 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 7101 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 7101 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 10061 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 10061 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 10061 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 10061 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 10061 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 6927 72 125I-Mel -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-Mel -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-Mel -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-Mel -23442 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 6929 121 125I-Iodomelatonin -14791 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 125I-Iodomelatonin -14791 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 125I-Iodomelatonin -14791 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
4209 9937 75 125I-Mel -26915 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 9937 75 125I-Mel -26915 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 9937 75 125I-Mel -26915 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 9937 75 125I-Mel -26915 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 9937 75 125I-Mel -26915 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 9937 75 125I-Mel -26915 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9166 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 9166 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 9166 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 120120 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 120120 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 8630 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 8630 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 222881 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 119678 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 119678 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 9166 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 9166 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 9166 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 6912 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 6912 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 6912 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 222878 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 222878 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 8247 72 None -38 38 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 8247 72 None -38 38 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 8247 72 None -38 38 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 8247 72 None -38 38 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 8247 72 None -38 38 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 222882 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 9166 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 9166 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 9166 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 119678 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 119678 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 120120 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 120120 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 10528 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 10528 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 10528 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 10528 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 10528 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 222878 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 7101 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 8314 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 8314 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 8314 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 6866 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 6866 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 6866 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 8198 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 8198 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 8198 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 6858 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 6858 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 6858 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 6858 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 6858 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 6858 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 6858 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 6858 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 10061 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 10061 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 10061 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 10061 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 10061 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 8767 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 8767 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 9166 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 9166 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 9166 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 9166 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 9166 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 9166 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 9166 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 9166 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 9166 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 9166 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 9166 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 9166 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 10687 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 10687 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 10686 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 10686 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 10686 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 10686 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 10686 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 10686 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 6948 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 7004 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 7004 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 7004 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 6950 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 6950 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 6950 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 6950 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 6950 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 6950 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 6950 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 6950 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 6950 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 6950 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 6950 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 6950 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 10689 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 10689 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 10689 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 10683 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 10683 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 10683 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 7601 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 7601 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 7601 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 9263 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 10528 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 10528 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 10528 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 10528 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 10528 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 21193 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 21193 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 9174 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 9174 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 9174 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 10206 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 10206 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 10206 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 6912 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 6912 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 6912 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 6912 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 6912 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 6912 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 6912 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 6912 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 6912 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 8626 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 8626 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 8626 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 8626 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 8626 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 8626 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 10209 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 10209 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 10209 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 8951 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 8951 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 8951 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 10208 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 10208 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 10208 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 6925 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 6925 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 6925 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 10207 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 10207 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 8771 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 8771 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 8771 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 10210 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 10210 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 10210 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 10211 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 10211 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 10211 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 8630 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 8630 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 8630 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 8630 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