Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
57781216 125326 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 125326 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 1503 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 1503 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 1503 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 2450 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
1672 2450 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
224 2450 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
896 2450 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
CHEMBL45 2450 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
DB01065 2450 133 None 1 3 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c01836
1357 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
1672 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
224 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
896 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
CHEMBL45 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
DB01065 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200221q
1357 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
1672 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
224 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
896 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
CHEMBL45 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
DB01065 2450 133 None 1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm200385u
139451757 184248 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 184248 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 184014 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 184014 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 184275 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 184275 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 184747 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 184747 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 184421 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 184421 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 185685 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 185685 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 166114 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 166114 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 184714 13 None 6 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859295 184714 13 None 6 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
1357 2450 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
1672 2450 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
224 2450 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
896 2450 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
CHEMBL45 2450 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
DB01065 2450 133 None 1 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.2c00717
1357 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1672 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
224 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
896 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
CHEMBL45 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
DB01065 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1357 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
1672 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
224 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
896 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
CHEMBL45 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
DB01065 2450 133 None 1 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/acs.jmedchem.0c00627
139451757 184248 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 184248 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 185751 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 185751 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 99654 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 99654 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 184014 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 184014 0 None 4 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 291 7 1 5 2.0 CCOc1nc2ccc(OC)cc2n1CCCNC(C)=O 10.1021/acs.jmedchem.0c00627
198 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
82148 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
99 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
CHEMBL10878 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
DB06594 310 120 None -3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
145982070 165922 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 165922 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 166198 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 166198 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 184421 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 184421 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 184428 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 184428 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 185257 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 185257 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 184714 13 None 6 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859295 184714 13 None 6 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysisAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in cAMP levels incubated at 28 degreeC by cellular dielectric spectroscopic analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
164946945 189635 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 189635 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 184275 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 184275 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 184747 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 184747 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 185685 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 185685 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 191920 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 191920 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 61690 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 61690 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 191920 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 191920 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 66593 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 66593 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 189554 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 189554 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 185362 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 185362 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 158973 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 158973 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 165937 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 165937 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 166728 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 166728 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 122647 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 122647 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 183865 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 183865 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 185560 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 185560 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 2450 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
1672 2450 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
224 2450 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
896 2450 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
CHEMBL45 2450 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
DB01065 2450 133 None 1 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assayAgonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2019.06.008
127026427 137159 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 137159 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 137295 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 137295 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 189554 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 189554 0 None 17 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
ChEMBL 411 7 1 7 3.4 COc1ccc2c(c1)c(CCNC(C)=O)cn2C(=O)OCc1ccccc1[N+](=O)[O-] 10.1021/acs.jmedchem.2c00717
198 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
82148 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
99 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
CHEMBL10878 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
DB06594 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
198 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
198 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
82148 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
82148 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
99 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
99 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
CHEMBL10878 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
CHEMBL10878 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
DB06594 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
DB06594 310 120 None -3 2 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assayIntrinsic activity at human MT1 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
1357 2450 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
1672 2450 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
224 2450 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
896 2450 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
CHEMBL45 2450 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
DB01065 2450 133 None 1 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmcl.2011.02.097
198 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
82148 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
99 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
CHEMBL10878 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
DB06594 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
198 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
82148 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
99 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
CHEMBL10878 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
DB06594 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
198 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
82148 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
99 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
CHEMBL10878 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
DB06594 310 120 None -3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2010.04.008
122188346 122646 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 122646 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 184428 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 184428 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 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
1672 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
224 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
896 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
CHEMBL45 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
DB01065 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
18360658 8802 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 8802 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 166122 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 166122 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 166666 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 166666 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 159128 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 159128 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 166238 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 166238 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 166359 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 166359 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 155836 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 155836 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 8755 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 8755 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 122632 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 122632 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 28702 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 28702 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 8556 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 8556 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 60428 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 60428 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 111744 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 111744 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 189635 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 189635 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 166504 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 166504 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 60440 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 60440 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 8780 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 8780 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 86646 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 86646 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 122631 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 122631 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 156310 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 156310 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 42974 37 None -2 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 308 5 2 2 3.5 COc1ccc2[nH]c(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1039/d2md00156j
CHEMBL15060 42974 37 None -2 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 308 5 2 2 3.5 COc1ccc2[nH]c(-c3ccccc3)c(CCNC(C)=O)c2c1 10.1039/d2md00156j
121231413 3846 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 3846 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 3846 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 62079 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 62079 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 157401 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 157401 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 156576 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 156576 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 122638 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 122638 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 165944 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 165944 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 122649 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 122649 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 60431 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 60431 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 183865 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 183865 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 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
1672 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
224 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
896 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
CHEMBL45 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
DB01065 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.bmc.2010.04.008
1357 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
1672 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
224 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
896 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
CHEMBL45 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
DB01065 2450 133 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1AAgonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0255872
10163052 8436 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 8436 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 8583 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 8583 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 8801 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 8801 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 8557 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 8557 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 86647 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 86647 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 166479 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 166479 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 166567 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 166567 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 155705 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 155705 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 62072 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 62072 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 120806 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 120806 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 111830 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 111830 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 8558 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 8558 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 190376 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 190376 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 8578 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 8578 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 62071 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 62071 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 122627 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 122627 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 122629 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 122629 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 206238 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 206238 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 158349 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 158349 1 None -39 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
ChEMBL 291 6 2 3 2.0 COc1ccc2cccc(C(CO)CNC(=O)CF)c2c1 10.1039/C4MD00149D
145 140 48 None -144 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1832 140 48 None -144 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
CHEMBL7257 140 48 None -144 11 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assayAgonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
DB14010 140 48 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 104740 90 None 1 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate ReaderAgonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate Reader
ChEMBL 290 1 5 6 1.5 Oc1cc(O)c2c(c1)O[C@H](c1ccc(O)c(O)c1)[C@@H](O)C2 10.1016/j.ejmech.2020.112960
CHEMBL311498 104740 90 None 1 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate ReaderAgonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate Reader
ChEMBL 290 1 5 6 1.5 Oc1cc(O)c2c(c1)O[C@H](c1ccc(O)c(O)c1)[C@@H](O)C2 10.1016/j.ejmech.2020.112960
7778 801 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 801 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 801 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 180150 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 180150 0 None -3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assayAgonist activity at human MT1 expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay
ChEMBL 245 4 1 4 1.3 COc1ccc2ncnc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2020.112078
198 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
82148 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
99 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
CHEMBL10878 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
DB06594 310 120 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysisAgonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/d2md00156j
122188229 122630 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 122630 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 120803 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 120803 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 137213 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 137213 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 166004 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 166004 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 61699 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 61699 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 8577 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 8577 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 184813 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 184813 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 166817 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 166817 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 156963 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 156963 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 122637 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 122637 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 60439 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 60439 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 179495 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 179495 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 120814 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 120814 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 122636 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 122636 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 3380 3 None -51 2 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
9998187 3380 3 None -51 2 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
CHEMBL33549 3380 3 None -51 2 Human 7.4 pEC50 = 7.4 Functional
Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1AIntrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
86273226 120804 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 120804 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 156921 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 156921 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 122633 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 122633 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 166058 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 166058 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 60429 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 60429 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 921 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 921 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 921 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 137294 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 137294 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 137109 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 137109 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 697 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 697 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 697 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 182176 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 182176 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 180340 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 180340 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 8480 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 8480 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 158527 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 158527 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 111842 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 111842 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 166004 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 166004 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 166376 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 166376 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 166683 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 166683 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 60430 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 60430 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 137275 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 137275 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 120805 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 120805 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 166070 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 166070 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 122650 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 122650 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 156970 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 156970 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 179558 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 179558 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 137164 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 137164 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 8627 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 8627 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 165878 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 165878 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 120809 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 120809 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 29686 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 29686 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 3383 3 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
9806449 3383 3 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
CHEMBL14453 3383 3 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assayAgonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
127025786 137324 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 137324 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 157634 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 157634 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 166122 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 166122 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 137206 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 137206 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 86645 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 86645 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 122651 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 122651 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 166637 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 166637 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 86643 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 86643 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 8628 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 8628 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 137208 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 137208 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 155545 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 155545 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 158339 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 158339 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 122626 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 122626 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 73798 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 73798 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 60438 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 60438 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 120811 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 120811 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 120807 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 120807 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 194027 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 194027 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 110378 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 110378 0 None - 0 Human 9.7 pKi = 9.7 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 330 5 2 4 2.5 CCOC(=O)c1[nH]c2ccc(OC)c3c2c1[C@@H](CNC(C)=O)CC3 10.1021/jm401343c
24763223 214 0 None - 0 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1021/jm401343c
8289 214 0 None - 0 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1021/jm401343c
CHEMBL3260987 214 0 None - 0 Human 8.9 pKi = 8.9 Functional
Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1021/jm401343c
52918077 60429 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 60429 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 3851 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assayAntagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm401343c
7772 3851 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assayAntagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm401343c
CHEMBL189449 3851 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assayAntagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm401343c
1357 2450 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 2450 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 2450 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 2450 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 2450 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 2450 133 None 1 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
103828029 3856 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 3856 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 3857 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 3857 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 3855 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 3855 0 None 50 2 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 3 4.2 CC(c1ccc(cc1)CNc1cccc(c1)c1[nH]cnn1)C 32040955
23581869 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None
7712 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None
CHEMBL1783282 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None
DB13994 548 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 5 2 5 3.2 CCCNC(=O)c1nnc2c(c1N)cccc2c1c(F)cccc1OC None




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10440 2642 15 None -21 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2642 15 None -21 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2642 15 None -21 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
122178509 120814 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 120814 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 30750 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 30750 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 111830 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 111830 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 125331 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 125331 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 125329 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 125329 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 125333 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 125333 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 125326 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 125326 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 125323 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 125323 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 160289 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 160289 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 125339 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 125339 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 125328 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 125328 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 125325 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 125325 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 125332 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 125332 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 9682 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 9682 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 161019 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 161019 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 160417 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 160417 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 125338 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 125338 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 160286 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 160286 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 97777 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 97777 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 116287 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 116287 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 160283 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 160283 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 125335 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 125335 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 125337 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 125337 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 109335 4 None 2 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL323332 109335 4 None 2 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
1357 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 125336 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 125336 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 28590 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 28590 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 28729 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 28729 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 109203 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 109203 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 174451 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 174451 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 125324 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 125324 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 Human 9.0 pIC50 = 9 Binding
Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Binding affinity for melatonin 1A receptor was measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm980026p
115348 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
1343 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
CHEMBL289233 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
DB08190 70 42 None 4 2 Human 9.0 pIC50 = 9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm980026p
9834952 29107 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 29107 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 141430 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 141430 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 8166 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 8166 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 9655 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 9655 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 9749 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 9749 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 162201 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 162201 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 109335 4 None 2 2 Human 8.8 pIC50 = 8.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
CHEMBL323332 109335 4 None 2 2 Human 8.8 pIC50 = 8.8 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm980026p
10061999 7955 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 7955 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 29637 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 29637 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 138131 6 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 2 2.9 CCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
CHEMBL37771 138131 6 None - 0 Human 8.7 pIC50 = 8.7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 257 5 1 2 2.9 CCC(=O)NCCc1cccc2ccc(OC)cc12 10.1021/jm980026p
10038961 9632 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 9632 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 29074 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 29074 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 118235 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 118235 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 188128 38 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
CHEMBL504585 188128 38 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.bmc.2008.03.036
3071635 9313 3 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 4 0 2 3.0 COc1ccc2cccc(CCN3CCCC3=O)c2c1 10.1021/jm980026p
CHEMBL111558 9313 3 None - 0 Human 7.0 pIC50 = 7 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 269 4 0 2 3.0 COc1ccc2cccc(CCN3CCCC3=O)c2c1 10.1021/jm980026p
21469690 28536 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 28536 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 118651 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 118651 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 188128 38 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
CHEMBL504585 188128 38 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to human MT1 receptorBinding affinity to human MT1 receptor
ChEMBL 275 4 3 3 2.0 COC(=O)Nc1ccc2[nH]cc(CCNC(C)=O)c2c1 10.1016/j.ejmech.2011.02.010
18177433 29182 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 29182 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 118365 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 118365 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 164496 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 164496 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 28704 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 28704 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 29090 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 29090 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 29279 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 29279 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 29324 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 29324 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 30036 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 30036 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 30419 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 30419 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 31490 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 31490 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 118746 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 118746 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 99739 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 99739 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 118716 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 118716 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 125330 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 125330 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 69485 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 69485 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 30194 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 30194 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 30499 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 30499 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 116033 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 116033 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 118501 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 118501 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 118924 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 118924 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 192505 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 192505 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 28678 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 28678 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 28702 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 28702 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 31833 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 31833 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 118873 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 118873 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 164704 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 164704 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 26656 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 26656 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 29466 3 None - 0 Human 4.9 pIC50 = 4.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 203 3 2 2 1.2 CC(=O)NCCc1c[nH]c2ncccc12 10.1021/jm980026p
CHEMBL138631 29466 3 None - 0 Human 4.9 pIC50 = 4.9 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 203 3 2 2 1.2 CC(=O)NCCc1c[nH]c2ncccc12 10.1021/jm980026p
23725513 125327 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 125327 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 9773 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 9773 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 28718 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 28718 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 28776 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 28776 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 28798 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 28798 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 28977 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 28977 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 161122 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 161122 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 69150 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 69150 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 26503 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 26503 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 27210 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 27210 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 169868 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 169868 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 29648 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 29648 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 32982 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 32982 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 118638 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 118638 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 118895 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 118895 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 167890 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 167890 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 28951 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 28951 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 29954 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 29954 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 32579 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 32579 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 66922 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 66922 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 9996 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 9996 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 188200 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 188200 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 125334 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 125334 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 28679 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 28679 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 29312 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 29312 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 29686 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 29686 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 29688 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 29688 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 29845 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 29845 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 118939 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 118939 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 27211 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 27211 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 29144 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 29144 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 32683 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 32683 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 119510 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 119510 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 110377 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 110377 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 29700 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 29700 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 137711 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 5 1 2 3.2 COc1ccc2cccc(CCNC(=O)C(C)C)c2c1 10.1021/jm980026p
CHEMBL37703 137711 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 271 5 1 2 3.2 COc1ccc2cccc(CCNC(=O)C(C)C)c2c1 10.1021/jm980026p
10266979 98562 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 98562 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 66671 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 66671 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 9329 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 9329 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 29959 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 29959 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 31383 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 31383 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 30428 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 30428 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 118821 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 118821 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 135821 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 344 5 2 2 4.3 COc1ccc2cccc(CCNC(=O)c3cc4ccccc4[nH]3)c2c1 10.1021/jm980026p
CHEMBL37341 135821 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 344 5 2 2 4.3 COc1ccc2cccc(CCNC(=O)c3cc4ccccc4[nH]3)c2c1 10.1021/jm980026p
18175032 175023 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 175023 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 186789 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 186789 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 31492 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 31492 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 32191 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 32191 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 168041 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 168041 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 108717 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 108717 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 114991 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 114991 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 116256 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 116256 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 168753 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 168753 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 174922 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 174922 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 30494 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 30494 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 31181 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 31181 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 9705 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 9705 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 30089 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 30089 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 118922 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 118922 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 186976 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 186976 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 8352 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 8352 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 29400 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 29400 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 30576 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 30576 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 31389 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 31389 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 116294 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 116294 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 118242 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 118242 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 99619 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 99619 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 71361 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 71361 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 175126 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 175126 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 9214 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 9214 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 28627 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 28627 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 29244 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 29244 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 29622 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 29622 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 108078 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 108078 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 29734 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 29734 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 118293 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 118293 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 118537 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 118537 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 118778 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 118778 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 118868 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 118868 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 59764 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 59764 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 29293 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 29293 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 29527 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 29527 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 29862 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 29862 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 31921 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 31921 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 33000 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 33000 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 66564 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 66564 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 186787 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 186787 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 192054 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 192054 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 9342 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 9342 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 29951 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 29951 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 30411 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 30411 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 125286 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 125286 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 28954 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 28954 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 118641 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 118641 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 31559 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 31559 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 32302 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 32302 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 116288 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 116288 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 31843 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 256 4 2 1 3.0 O=C(NCCc1c[nH]c2ccccc12)C1CCCC1 10.1021/jm980026p
CHEMBL140835 31843 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL 256 4 2 1 3.0 O=C(NCCc1c[nH]c2ccccc12)C1CCCC1 10.1021/jm980026p
588712 32877 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 32877 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 167656 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 167656 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 29369 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 29369 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 115902 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 115902 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 118472 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 118472 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 118538 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 118538 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 118838 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 118838 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 174412 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 174412 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 29852 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 29852 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 31493 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 31493 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 32669 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 32669 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 118273 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 118273 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 30664 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 30664 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 118835 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 118835 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 30031 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 30031 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 187112 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 187112 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 61076 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 61076 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2642 15 None -21 3 Human 5.2 pKd = 5.2 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
139030523 2642 15 None -21 3 Human 5.2 pKd = 5.2 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
CHEMBL4449712 2642 15 None -21 3 Human 5.2 pKd = 5.2 Binding
Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay
ChEMBL 417 7 3 7 4.2 OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F 10.1021/acs.jmedchem.9b00869
22004862 61693 0 None -1 2 Human 11.1 pKi = 11.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 319 4 1 2 3.6 CC(=O)NCCC1=C(c2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200385u
CHEMBL1774522 61693 0 None -1 2 Human 11.1 pKi = 11.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 319 4 1 2 3.6 CC(=O)NCCC1=C(c2ccccc2)Cc2ccc3c(c21)CCO3 10.1021/jm200385u
9903515 22591 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 22591 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 99654 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 99654 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 112088 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 112088 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 99654 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 99654 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 115936 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 115936 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 61686 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 61686 0 None -1 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 299 5 1 2 3.5 CCC(=O)NCCC1=C(C(C)C)Cc2ccc3c(c21)CCO3 10.1021/jm200221q
115348 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
1343 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
CHEMBL289233 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
DB08190 70 42 None 4 2 Human 10.9 pKi = 10.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm011053+
1356 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
208902 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
2355 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
CHEMBL1218 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
DB00980 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity against human Melatonin receptor type 1A (MT1)Binding affinity against human Melatonin receptor type 1A (MT1)
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/jm0201159
1356 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
208902 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
2355 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
CHEMBL1218 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
DB00980 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
Binding affinity to human MT1 expressed in CHO cellsBinding affinity to human MT1 expressed in CHO cells
ChEMBL 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 10.1021/acs.jmedchem.0c01836
9926304 116075 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 116075 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 117650 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 117650 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 106395 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 106395 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 61685 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 61685 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 23360 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 23360 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 63466 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 63466 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 185313 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 185313 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 35611 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 35611 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 19645 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 19645 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 122646 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 122646 0 None - 1 Human 10.5 pKi = 10.5 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor transfected in CHO cell membranes after 120 mins
ChEMBL 262 4 1 3 2.0 CCC(=O)NCC1CCc2c(OC)cccc2N1C 10.1021/acs.jmedchem.5b01066
71533431 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 10.1016/j.bmcl.2012.11.069
7775 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 10.1016/j.bmcl.2012.11.069
CHEMBL2314259 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 10.1016/j.bmcl.2012.11.069
57781216 125326 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 125326 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 61688 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 61688 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 125332 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 125332 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 63464 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 63464 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 205831 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 205831 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 64658 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 64658 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 137547 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 137547 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 85987 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 85987 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 63465 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 63465 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 61684 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 61684 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 32493 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 32493 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 97704 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 97704 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 203906 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 203906 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 67258 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 67258 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 78379 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 78379 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 78384 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 78384 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 78388 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 78388 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 78389 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 78389 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 78390 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 78390 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 78394 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 78394 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 1388 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 1388 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 1388 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 1388 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 1388 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 1388 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 19285 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 19285 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 61696 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 61696 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation countingDisplacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting
ChEMBL 349 5 1 3 3.6 COc1cccc(C2=C(CCNC(C)=O)c3c(ccc4c3CCO4)C2)c1 10.1021/jm200221q
198 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
82148 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
99 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
CHEMBL10878 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
DB06594 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm0255872
198 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
82148 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
99 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
CHEMBL10878 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmc.2008.08.052
DB06594 310 120 None -1 5 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 85985 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 85985 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 1503 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 1503 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 1503 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 125325 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 125325 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 125328 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 125328 0 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cell membrane incubated for 150 mins by radioligand binding assay
ChEMBL 272 4 1 3 3.1 CCC(=O)NCCC1CCc2ccc3nc(C)oc3c21 10.1021/acs.jmedchem.0c01836
115348 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
1343 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
CHEMBL289233 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
DB08190 70 42 None 4 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1021/jm401343c
53238185 61694 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 61694 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 116154 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 116154 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 8557 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 8557 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 2363 15 None -1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 10.1039/C4MD00149D
219018 2363 15 None -1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 10.1039/C4MD00149D
CHEMBL4079759 2363 15 None -1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to MT1 receptor (unknown origin)Binding affinity to MT1 receptor (unknown origin)
ChEMBL 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 10.1039/C4MD00149D
9893513 30745 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 30745 0 None 29 2 Human 10.1 pKi = 10.1 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 540 15 2 4 6.4 CC(=O)NCCc1cccc2ccc(OCCCCCCOc3ccc4cccc(CCNC(C)=O)c4c3)cc12 10.1021/jm0255872
115348 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
1343 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
CHEMBL289233 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
DB08190 70 42 None 4 2 Human 10.1 pKi = 10.1 Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
ChEMBL 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 10.1016/S0960-894X(97)00444-7
11100761 101321 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 101321 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 63461 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 63461 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 63463 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 63463 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 8436 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 8436 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 100144 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 100144 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 100144 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 100144 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 20056 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 20056 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 22052 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 22052 0 None 3 2 Human 10.0 pKi = 10 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 283 4 1 2 3.4 COc1ccc2cccc3c2c1C(CCNC(C)=O)CC3 10.1021/jm000922c
198 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
82148 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
99 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
CHEMBL10878 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2017.10.025
DB06594 310 120 None -1 5 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 165922 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 165922 0 None 1 2 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 283 3 1 2 3.2 COc1ccc2ccc3c(c2c1)C(C)(CNC(C)=O)CC3 10.1016/j.ejmech.2017.10.025
198 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
82148 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
99 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
CHEMBL10878 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
DB06594 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2016.12.013
198 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
82148 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
99 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
CHEMBL10878 310 120 None -1 5 Human 10.0 pKi = 10 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma countingDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.bmcl.2012.11.069
DB06594 310 120 None -1 5 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 85988 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 85988 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 21163 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 21163 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 61687 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 61687 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 19995 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 19995 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 Human 9.9 pKi = 9.9 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm0005252
198 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
82148 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
99 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
CHEMBL10878 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2015.12.047
DB06594 310 120 None -1 5 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK or CHO cell membranes after 120 mins
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2016.12.013
198 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
82148 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
99 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
CHEMBL10878 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1016/j.ejmech.2020.112078
DB06594 310 120 None -1 5 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 Human 9.9 pKi = 9.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cellsInhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells
ChEMBL 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1021/jm011053+
198 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
82148 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
99 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
CHEMBL10878 310 120 None -1 5 Human 9.9 pKi = 9.9 Binding
Displacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1039/C4MD00149D
DB06594 310 120 None -1 5 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 66986 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 66986 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 26870 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 26870 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 109335 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm0005252
CHEMBL323332 109335 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1021/jm0005252
56653119 171226 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 171226 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 109335 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2015.12.047
CHEMBL323332 109335 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 minsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2015.12.047
10059864 109335 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2016.01.008
CHEMBL323332 109335 4 None 2 2 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 1 3 2.1 COc1ccc2occ(CCNC(C)=O)c2c1 10.1016/j.ejmech.2016.01.008
24954991 63462 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 63462 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 185733 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 185733 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 118781 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 118781 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells.
ChEMBL 260 3 1 3 1.7 CCC(=O)N[C@H]1CCN(c2cccc3c2CCO3)C1 10.1016/j.bmcl.2003.09.030
198 310 120 None -1 5 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
82148 310 120 None -1 5 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
99 310 120 None -1 5 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
CHEMBL10878 310 120 None -1 5 Human 9.7 pKi = 9.7 Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 10.1021/jm000922c
DB06594 310 120 None -1 5 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 98456 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 98456 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 19284 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 19284 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 20504 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 20504 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 167316 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 167316 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 60428 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 60428 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 185690 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 185690 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 137385 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 137385 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 137532 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 137532 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 85990 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 85990 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 116128 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 116128 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 98150 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 98150 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 125335 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 125335 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 60428 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 60428 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 60428 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 60428 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 8627 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 8627 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 165944 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 165944 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 166728 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 166728 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 158973 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 158973 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 185337 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 185337 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 85983 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 85983 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 192900 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 192900 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 63468 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 63468 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 184275 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 184275 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 67186 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 67186 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 185594 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 185594 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 19645 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 19645 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 167761 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 167761 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 8558 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 8558 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 185751 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 185751 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 203795 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 203795 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 125336 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 125336 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 166004 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 166004 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 166114 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 166114 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 19635 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 19635 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 184747 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 184747 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 21163 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 21163 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 125324 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 125324 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 125337 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 125337 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 63467 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 63467 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 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
9870523 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
CHEMBL429392 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
1362 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9870523 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL429392 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
1362 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9870523 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL429392 3382 18 None 39 2 Human 9.3 pKi = 9.3 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
1357 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 801 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 801 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 801 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 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
9806449 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
CHEMBL14453 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm0255872
1355 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9806449 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL14453 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to MT1 receptor (unknown origin) expressed in HEK cellsBinding affinity to MT1 receptor (unknown origin) expressed in HEK cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
44272425 66990 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 66990 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 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9806449 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL14453 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
145982333 166004 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 166004 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 166469 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 166469 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 166683 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 166683 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 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
9806449 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
CHEMBL14453 3383 3 None 70 2 Human 9.2 pKi = 9.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1016/j.bmc.2010.04.008
137647756 157401 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 157401 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 185685 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 185685 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 114313 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 114313 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 114313 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 114313 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 8755 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 8755 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 26911 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 26911 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 21282 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 21282 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 18363 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 18363 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 122647 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 122647 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 185362 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 185362 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 15703 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 15703 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 205892 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 205892 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 112373 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 112373 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 3848 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 3848 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 3848 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 116311 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 116311 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 8556 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 8556 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 116093 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 116093 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 166058 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 166058 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 166376 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 166376 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 155545 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 155545 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 3854 10 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 10.1021/jm700957j
7777 3854 10 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 10.1021/jm700957j
CHEMBL237236 3854 10 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 10.1021/jm700957j
24750193 88125 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 88125 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 184248 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 184248 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 61691 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 61691 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 28740 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 28740 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 8780 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 8780 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 15701 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 15701 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 68334 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 68334 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 20475 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 20475 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 67674 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 67674 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 62673 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 62673 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 121827 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 121827 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 122759 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 122759 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 129648 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 129648 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 203469 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 203469 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 185257 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 185257 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 166070 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 166070 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 166198 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 166198 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 206054 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 206054 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 8779 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 8779 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 117987 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 117987 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 8628 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 8628 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 96549 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 96549 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 184014 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 184014 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 185560 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 185560 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 61689 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 61689 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 61695 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 61695 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 193554 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 193554 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 76349 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 76349 1 None 2 2 Human 9.0 pKi = 9.0 Binding
Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells
ChEMBL 260 4 2 2 2.6 COc1ccc2[nH]cc(C(C)(C)CNC(C)=O)c2c1 10.1021/jm0512544
24763223 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 mins
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1039/C5MD00190K
8289 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 mins
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1039/C5MD00190K
CHEMBL3260987 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 mins
ChEMBL 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 10.1039/C5MD00190K
20642483 30437 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 30437 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 19786 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 19786 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 110379 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 110379 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 184421 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 184421 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 136325 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 136325 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 183980 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 183980 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 77895 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 77895 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 136325 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 136325 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 189635 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 189635 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 111830 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 111830 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 111830 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 111830 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 111830 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 111830 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 67153 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 67153 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 116584 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 116584 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 167982 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 167982 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 116414 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 116414 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 69966 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 69966 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 60431 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 60431 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 185039 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 185039 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 61701 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 61701 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 24533 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 24533 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 114858 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 114858 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 110376 5 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 280 4 2 2 2.8 COc1cc2c(CCNC(C)=O)c(C)[nH]c2cc1Cl 10.1021/jm401343c
CHEMBL3260979 110376 5 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 280 4 2 2 2.8 COc1cc2c(CCNC(C)=O)c(C)[nH]c2cc1Cl 10.1021/jm401343c
10244841 67155 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 67155 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 158527 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 158527 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 8801 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 8801 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 60429 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 60429 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 67155 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 67155 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 61700 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 61700 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 173650 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 173650 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 116040 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 116040 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 8578 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 8578 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 156537 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 156537 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 122650 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 122650 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 137372 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 137372 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 77731 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 77731 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 15674 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 15674 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 149690 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 149690 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 193815 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 193815 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 206337 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 206337 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 191920 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 191920 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 116092 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 116092 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 137159 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 137159 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 159128 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 159128 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 20401 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 20401 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 137167 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 137167 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 123888 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 123888 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 86935 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 86935 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 76761 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 76761 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 203514 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 203514 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 29686 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 29686 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 203583 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 203583 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 148712 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 148712 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 174105 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 174105 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 194597 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 194597 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 174105 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 174105 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells
ChEMBL 345 3 1 3 3.3 CC(=O)NCCc1c2n(c3ccccc13)CC1Cc3ccccc3N1C2 10.1016/j.bmc.2008.07.012
25210130 69 0 None -91 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
7782 69 0 None -91 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
CHEMBL514415 69 0 None -91 2 Human 7.0 pKi = 7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
1358 124 35 None -870 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm048956y
3976006 124 35 None -870 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm048956y
CHEMBL285718 124 35 None -870 2 Human 7.0 pKi = 7.0 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm048956y
54584155 60432 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 60432 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 15655 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 15655 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 65957 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 65957 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 203661 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 203661 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 101341 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 101341 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 174352 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 174352 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 174352 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 174352 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 194888 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 194888 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 15675 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 15675 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 65814 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 65814 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 21580 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 21580 0 None -6 2 Human 8.0 pKi = 8.0 Binding
Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cellsInhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells
ChEMBL 349 7 1 4 3.1 CCC(=O)NCCc1c(OC(=O)CCl)ccc2ccc(OC)cc12 10.1021/jm970437q
1346 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1016/j.ejmech.2019.111847
1858 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1016/j.ejmech.2019.111847
CHEMBL34730 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1016/j.ejmech.2019.111847
1346 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1021/jm401343c
1858 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1021/jm401343c
CHEMBL34730 160 42 None -25 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 10.1021/jm401343c
11587169 76964 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 76964 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 136166 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 136166 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 195070 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 195070 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 68733 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 68733 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 64659 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 64659 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 194888 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 194888 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 3382 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9870523 3382 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL429392 3382 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
11403195 123162 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 123162 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 108898 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 108898 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 3382 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
9870523 3382 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
CHEMBL429392 3382 18 None 39 2 Human 7.0 pKi = 7.0 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysisDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1039/C5MD00190K
25210130 69 0 None -91 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
7782 69 0 None -91 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
CHEMBL514415 69 0 None -91 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 363 6 2 3 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)CN1CCc2c1cccc2 10.1021/jm800974d
16743124 91777 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 91777 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 180861 2 None -10 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1nncc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
CHEMBL4764211 180861 2 None -10 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assayDisplacement of 2-[125l]-lodomelatonin from human MT1 expressed in CHO cells incubated for 120 mins by radioligand binding assay
ChEMBL 273 6 1 4 2.1 CCCC(=O)NCCc1nncc2ccc(OC)cc12 10.1016/j.ejmech.2020.112078
12436516 15680 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 15680 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 15758 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 15758 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 206442 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 206442 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 122629 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 122629 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 16345 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 16345 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 76771 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 76771 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 206370 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 206370 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 7624 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 7624 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 16595 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 16595 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 203154 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 203154 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 136166 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 136166 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 163666 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 163666 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 206109 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 206109 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 137461 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 137461 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 189032 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 189032 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 15718 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 15718 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 206596 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 206596 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 82859 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 82859 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 15751 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 15751 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 15757 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 15757 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 189032 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 189032 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 86643 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 86643 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 60435 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 60435 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 122639 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 122639 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 206634 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 206634 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 206634 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 206634 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 158576 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 158576 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 181548 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 181548 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 190035 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 190035 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 89455 2 None -32 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 254 5 1 2 3.0 CC(=O)NCCN(c1ccccc1)c1ccccc1 10.1021/jm700957j
CHEMBL237840 89455 2 None -32 2 Human 6.9 pKi = 6.9 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 254 5 1 2 3.0 CC(=O)NCCN(c1ccccc1)c1ccccc1 10.1021/jm700957j
44429455 87320 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 87320 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 181249 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 181249 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 8171 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 8171 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 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm001125h
7783 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm001125h
CHEMBL33185 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligandBinding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm001125h
10903368 206364 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 206364 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 193099 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 193099 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 88126 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 88126 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 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm048956y
7783 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm048956y
CHEMBL33185 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm048956y
44429452 86937 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 86937 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 115913 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 115913 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 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human MT1 receptorAntagonist activity at human MT1 receptor
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm401343c
7783 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human MT1 receptorAntagonist activity at human MT1 receptor
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm401343c
CHEMBL33185 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Antagonist activity at human MT1 receptorAntagonist activity at human MT1 receptor
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm401343c
10428383 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm800974d
7783 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm800974d
CHEMBL33185 3850 3 None -151 2 Human 5.9 pKi = 5.9 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 356 6 1 3 4.4 CCC(=O)NCc1cc2c(n1Cc1ccc(cc1)Cl)cccc2OC 10.1021/jm800974d
139451766 183865 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 183865 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 122627 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 122627 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 123424 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 123424 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 61699 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 61699 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 16708 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 16708 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 96097 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 96097 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 89050 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 89050 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 122633 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 122633 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 174639 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 174639 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 206566 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 206566 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 206566 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 206566 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 86643 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 86643 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 86643 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 86643 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 186531 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 186531 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 15656 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 15656 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 181251 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 181251 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 120803 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 120803 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 86936 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 86936 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 112060 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 112060 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 64122 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 64122 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 206084 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 206084 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 101077 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 101077 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 137284 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 137284 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 170310 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 170310 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 118700 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 118700 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 118700 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 118700 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 170310 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 170310 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 16329 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 16329 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 8334 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 8334 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 188396 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 188396 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 189554 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 189554 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 179307 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 179307 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 97714 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 97714 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 188396 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 188396 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 138921 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 138921 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 194422 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 194422 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 87104 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 87104 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 181749 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 181749 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 165704 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 165704 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 168550 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 168550 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 137324 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 137324 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 137206 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 137206 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 2355 67 None -18 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm401343c
1363 2355 67 None -18 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm401343c
CHEMBL286615 2355 67 None -18 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm401343c
54581170 60439 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 60439 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 158785 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 158785 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 65993 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 65993 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 122195 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 122195 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 164061 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 164061 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of [125I]iodomelatonin from human MT1 receptor expressed in rat NIH/3T3 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 517 15 2 5 6.0 CCC(=O)NCCN(C)c1cccc(OCCCCCCNC(=O)Oc2cccc(-c3ccccc3)c2)c1 10.1021/acs.jmedchem.8b00893
10849065 137 8 None 4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
1345 137 8 None 4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
CHEMBL126809 137 8 None 4 2 Human 7.8 pKi = 7.8 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis
ChEMBL 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 10.1016/j.ejmech.2019.111847
24750191 88124 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 88124 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 66716 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 66716 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 108014 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 108014 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 108014 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 108014 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 16659 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 16659 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 3846 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 3846 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 3846 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 120805 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 120805 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 137207 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 137207 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 187567 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 187567 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 27309 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 27309 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 120809 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 120809 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 140529 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 140529 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 122648 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 122648 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 4608 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 4608 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 77640 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 77640 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 189135 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 189135 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 203321 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 203321 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 97861 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 97861 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 203275 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 203275 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 189135 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 189135 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 189135 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 189135 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 189135 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 189135 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 116468 1 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 308 5 1 3 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2-c1ccccc1 10.1021/jm020982d
CHEMBL33869 116468 1 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding Affinity (pKi) towards human Melatonin receptor type 1ABinding Affinity (pKi) towards human Melatonin receptor type 1A
ChEMBL 308 5 1 3 3.3 COc1ccc2c(c1)c(CCNC(C)=O)cn2-c1ccccc1 10.1021/jm020982d
90666303 108892 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 108892 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 156921 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 156921 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 206466 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 206466 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 206466 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 206466 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 189135 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 189135 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 16474 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 16474 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 8021 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 8021 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 8043 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 8043 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 122634 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 122634 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 163297 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 163297 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 101410 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 101410 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 155460 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 155460 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 85982 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 85982 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 126764 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 126764 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 148512 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 148512 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 192795 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 192795 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 146199 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 146199 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 64120 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 64120 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 91649 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 91649 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 102594 64 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 298 6 0 3 4.9 CC(C)=CCC/C(C)=C/COc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
CHEMBL307341 102594 64 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 298 6 0 3 4.9 CC(C)=CCC/C(C)=C/COc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
44349269 16411 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 16411 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 206324 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 206324 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 137500 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 137500 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 38983 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 38983 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 64501 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 64501 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 129456 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 129456 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 130852 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 130852 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 166283 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 166283 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 166567 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 166567 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 166637 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 166637 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 156310 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 156310 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 158339 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 158339 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 36732 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 36732 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 117607 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 117607 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 184714 13 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
CHEMBL4859295 184714 13 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysisDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 60 mins by scintillation counting analysis
ChEMBL 297 5 1 5 1.8 COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O 10.1021/acs.jmedchem.0c00627
127026062 137164 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 137164 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 66630 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 66630 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 118867 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 118867 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 202188 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 202188 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 184428 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 184428 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 168632 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 168632 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 137492 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 137492 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 116149 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 116149 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 116461 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 116461 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 189554 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 189554 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 8480 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 8480 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 156537 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 156537 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 66678 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 66678 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 120806 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 120806 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 116149 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 116149 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 66593 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 66593 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 22820 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 22820 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 82832 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 82832 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 86299 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 86299 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 61690 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 61690 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 16615 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 16615 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 137294 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 137294 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 144812 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 144812 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 21163 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 21163 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 155686 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 155686 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 137295 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 137295 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 63460 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 63460 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 84934 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 84934 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 64093 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 64093 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 8258 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 8258 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 26576 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 26576 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 96866 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 96866 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 186509 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 186509 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 206622 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 206622 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 125368 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 125368 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 16637 6 None -60 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 262 5 2 3 1.9 COc1cc2[nH]cc(CCNC(C)=O)c2cc1OC 10.1021/jm401343c
CHEMBL124699 16637 6 None -60 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 262 5 2 3 1.9 COc1cc2[nH]cc(CCNC(C)=O)c2cc1OC 10.1021/jm401343c
11287002 15753 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 15753 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 27305 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 27305 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 65785 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 65785 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 163704 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 163704 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 111744 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 111744 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 111744 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 111744 0 None -194 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 379 9 1 4 4.3 C=CCC(=O)NCCc1c(Cc2cccc(OC)c2)oc2ccc(OC)cc12 10.1021/jm401343c
145 140 48 None -40 29 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
1832 140 48 None -40 29 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
CHEMBL7257 140 48 None -40 29 Human 6.7 pKi = 6.7 Binding
Displacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 minsDisplacement of 2-[125I]-iodomelatonin from human melatonin receptor-1 transfected in CHO cell membranes after 120 mins
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/acs.jmedchem.5b00245
DB14010 140 48 None -40 29 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 120810 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 120810 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 137217 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 137217 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 180340 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 180340 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 180436 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 180436 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 77641 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 77641 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 122635 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 122635 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 84935 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 84935 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 82848 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 82848 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 138987 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 138987 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 155705 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 155705 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 122651 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 122651 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 66910 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 66910 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 62075 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 62075 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 182176 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 182176 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 86646 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 86646 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 99625 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 99625 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 62073 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 62073 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 170066 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 170066 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 165491 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 165491 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 170570 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 170570 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 125327 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 125327 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 65906 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 65906 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 188097 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 188097 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 137275 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 137275 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 108896 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 108896 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 82832 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 82832 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 180150 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 180150 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 206040 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 206040 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 62077 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 62077 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 123579 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 123579 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 206387 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 206387 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 114107 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 114107 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 106883 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 106883 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 141559 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 141559 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 62071 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 62071 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 186532 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 186532 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 97685 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 97685 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 206565 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 206565 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 206565 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 206565 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 159000 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 159000 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 85986 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 85986 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 136100 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 136100 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 83059 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 83059 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 96931 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 96931 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 108891 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 108891 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 209344 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 4109 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 4109 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 8106 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 8106 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 193196 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 193196 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 194351 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 194351 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 82833 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 82833 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 182730 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 182730 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 7990 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 7990 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 91894 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 91894 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 98041 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 98041 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 3380 3 None -112 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm800974d
9998187 3380 3 None -112 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm800974d
CHEMBL33549 3380 3 None -112 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm800974d
145976375 163245 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 163245 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 8245 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 8245 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 97967 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 97967 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 1925 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 1925 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 1925 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 206541 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 206541 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 15676 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 15676 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 157604 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 157604 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 64660 4 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 1 4 2.7 COc1ccc2nc(-c3ccccc3)c(CCNC(C)=O)n2c1 10.1016/j.ejmech.2011.06.030
CHEMBL1823017 64660 4 None -3 2 Human 7.6 pKi = 7.6 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assayDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay
ChEMBL 309 5 1 4 2.7 COc1ccc2nc(-c3ccccc3)c(CCNC(C)=O)n2c1 10.1016/j.ejmech.2011.06.030
86273223 120807 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 120807 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 108894 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 108894 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 15699 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 15699 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 97686 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 97686 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 62076 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 62076 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 206181 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 206181 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 97826 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 97826 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 64125 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 64125 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 205811 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 205811 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 203395 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 203395 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 165878 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 165878 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 158569 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 158569 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 163347 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 163347 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 122640 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 122640 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 8084 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 8084 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 206599 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 206599 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 206553 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 206553 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 206553 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 206553 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 180638 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 180638 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 18373 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 18373 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 166122 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 166122 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 61697 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 61697 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 165815 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 165815 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 156537 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 156537 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 15722 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 15722 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 68840 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 68840 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 3383 3 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9806449 3383 3 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL14453 3383 3 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
71540395 85989 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 85989 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 206193 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 206193 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 17099 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 17099 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 60430 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 60430 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 156576 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 156576 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 64119 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 64119 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 156067 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 156067 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 110379 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 110379 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 8802 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 8802 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 16584 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 16584 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 67604 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 67604 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 157297 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 157297 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 206238 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 206238 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 87318 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 87318 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 184813 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 184813 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 15657 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 15657 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 30478 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 30478 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 85984 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 85984 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 66722 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 66722 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 15725 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 15725 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 29004 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 29004 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 19645 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 19645 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 3382 18 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
9870523 3382 18 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
CHEMBL429392 3382 18 None 39 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 10.1021/jm401343c
56653120 110380 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 110380 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 64121 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 64121 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 16604 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 16604 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 96594 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 96594 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 188904 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 188904 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 188968 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 188968 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 140545 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 140545 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 181416 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 181416 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 122630 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 122630 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 140547 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 140547 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 206554 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 206554 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 188904 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 188904 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 163938 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 163938 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 202756 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 202756 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 137424 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 137424 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 206397 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 206397 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 163308 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 163308 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 158429 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 158429 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 188968 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 188968 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 206473 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 206473 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 15782 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 15782 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 188968 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 188968 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 166004 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 166004 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 209345 0 None -3 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 minsDisplacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells after 120 mins
ChEMBL None None None COc1ccc2c(c1)c(CCNC(C)=O)c1n2[B-](F)(F)[N+]2=C(C)C=C(C)C2=C1 10.1021/ml4004155
129776 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1016/j.ejmech.2019.111847
1364 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1016/j.ejmech.2019.111847
CHEMBL339105 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting methodDisplacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1016/j.ejmech.2019.111847
129776 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1021/jm401343c
1364 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1021/jm401343c
CHEMBL339105 142 5 None -128 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 322 6 2 2 3.4 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)Cc1ccccc1 10.1021/jm401343c
71508235 86647 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 86647 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 188968 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 188968 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 179558 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 179558 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 89518 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 89518 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 122652 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 122652 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 123155 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 123155 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 148680 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 148680 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 107067 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 107067 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 112593 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 112593 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 203139 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 203139 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 156202 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 156202 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 165210 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 165210 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 192781 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 192781 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 191920 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 191920 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 163656 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 163656 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 18367 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 18367 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 155836 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 155836 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 15756 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 15756 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 136128 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 136128 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 120814 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 120814 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 120814 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 120814 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 136128 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 136128 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 15754 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 15754 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 203434 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 203434 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 82849 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 82849 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 82872 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 82872 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 15700 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 15700 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 15755 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 15755 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 122636 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 122636 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 162470 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 162470 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 91871 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 91871 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 15784 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 15784 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 15679 35 None -5 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1ccccc1OCCNC(C)=O 10.1016/j.bmc.2010.06.100
CHEMBL1223055 15679 35 None -5 2 Human 4.4 pKi = 4.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 209 5 1 3 1.2 COc1ccccc1OCCNC(C)=O 10.1016/j.bmc.2010.06.100
46885230 8109 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 8109 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 174743 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 174743 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 174743 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 174743 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 86645 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 86645 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 186212 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 186212 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 164289 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 164289 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 64124 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 64124 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 106777 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 106777 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 106777 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 106777 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 15698 14 None -11 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 195 4 1 2 1.9 CC(=O)NCCSc1ccccc1 10.1016/j.bmc.2010.06.100
CHEMBL1223125 15698 14 None -11 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 minsDisplacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins
ChEMBL 195 4 1 2 1.9 CC(=O)NCCSc1ccccc1 10.1016/j.bmc.2010.06.100
44579261 186396 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 186396 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 141804 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 141804 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 206098 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 206098 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 125322 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 125322 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 80430 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 80430 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 121529 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 121529 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 697 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 697 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 697 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 206626 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 206626 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 206626 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 206626 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 64270 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 64270 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 123425 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 123425 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 166122 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 166122 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 166493 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 166493 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 166666 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 166666 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 156963 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 156963 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 8583 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 8583 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 4272 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 4272 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 4272 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 4272 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 88123 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 88123 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 98463 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 98463 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 87319 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 87319 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 15720 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 15720 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 21307 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 21307 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 137785 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 137785 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 203524 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 203524 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 116056 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 116056 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 97769 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 97769 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 118467 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 118467 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 185406 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 185406 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 1959 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 1959 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 1959 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 1959 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 1959 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 1959 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 17025 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 17025 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 137109 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 137109 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 158349 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 158349 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 162980 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 162980 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 67293 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 67293 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 166379 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 166379 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 139014 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 139014 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 16412 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 16412 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 17765 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 17765 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 28702 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 28702 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 28702 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 28702 1 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assayDisplacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay
ChEMBL 233 4 2 3 1.2 COc1c[nH]c2ncc(CCNC(C)=O)c-2c1 10.1016/j.ejmech.2016.01.008
1347 162 51 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10.1016/j.ejmech.2019.111847
1864 162 51 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10.1016/j.ejmech.2019.111847
CHEMBL127421 162 51 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to MT1 receptor (unknown origin) assessed as inhibition constantBinding affinity to MT1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10.1016/j.ejmech.2019.111847
1353 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
9998187 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
CHEMBL33549 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand.
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm0005252
1353 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm401343c
9998187 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm401343c
CHEMBL33549 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cellsDisplacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm401343c
25209861 174647 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 174647 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 188970 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 188970 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 150831 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 150831 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 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm048956y
9998187 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm048956y
CHEMBL33549 3380 3 None -112 2 Human 7.4 pKi = 7.4 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 10.1021/jm048956y
46885285 8083 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 8083 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 119184 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 119184 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 119184 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 119184 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 203909 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 203909 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 174647 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 174647 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 188970 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 188970 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 92757 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 92757 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 82920 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 82920 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 203801 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 203801 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 123706 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 123706 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 64116 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 64116 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 205844 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 205844 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 15654 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 15654 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 137242 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 137242 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 156454 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 156454 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 98094 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 98094 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 16397 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 16397 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 8213 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 8213 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 37496 23 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 252 3 0 3 3.4 O=c1ccc2ccc(OCc3ccccc3)cc2o1 10.1021/acs.jnatprod.7b00853
CHEMBL145781 37496 23 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 252 3 0 3 3.4 O=c1ccc2ccc(OCc3ccccc3)cc2o1 10.1021/acs.jnatprod.7b00853
145965883 163530 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 163530 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 122637 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 122637 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 122638 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 122638 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 4292 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 4292 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 76348 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 76348 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 111033 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 111033 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 189635 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 189635 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 15759 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 15759 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 76889 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 76889 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 15673 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 15673 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 122628 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 122628 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 138928 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 138928 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 16239 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 16239 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 209343 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 101411 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 101411 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 29750 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 29750 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 181547 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 181547 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 18362 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 18362 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 138150 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 138150 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 122631 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 122631 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 109155 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 109155 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 136349 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 136349 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 120804 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 120804 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 165868 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 165868 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 166817 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 166817 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 157847 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 157847 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 136349 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 136349 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 98401 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 98401 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 86934 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 86934 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 8804 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 8804 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 8804 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 8804 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 153019 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 153019 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 122632 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 122632 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 205741 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 205741 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 15719 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 15719 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 77895 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 77895 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 108895 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 108895 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 137208 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 137208 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 109155 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 109155 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 189150 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 189150 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 15677 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 15677 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 122649 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 122649 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 189150 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 189150 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 157634 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 157634 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 206700 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 206700 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 202285 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 202285 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 189642 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 189642 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 16736 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 16736 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 206623 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 206623 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 149950 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 149950 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 186397 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 186397 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 113651 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 113651 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 179495 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 179495 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 4311 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 4311 0 None -41 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 374 5 1 3 4.3 COc1ccc2c(c1)c(CCNC(=O)C1CC1)c1n2CCCc2ccccc2-1 10.1021/jm980684+
1358 124 35 None -870 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm401343c
3976006 124 35 None -870 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm401343c
CHEMBL285718 124 35 None -870 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm401343c
22718661 16660 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 16660 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 191025 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 191025 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 60433 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 60433 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 82901 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 82901 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 97869 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 97869 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 4564 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 4564 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 62079 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 62079 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 49459 42 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 230 3 0 3 3.1 CC(C)=CCOc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
CHEMBL156692 49459 42 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysisDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cell lysates after 1 hr by gamma counting analysis
ChEMBL 230 3 0 3 3.1 CC(C)=CCOc1ccc2ccc(=O)oc2c1 10.1021/acs.jnatprod.7b00853
10563168 119187 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 119187 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 119187 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 119187 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 83065 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 83065 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 172961 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 172961 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 206140 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 206140 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 168785 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 168785 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 15697 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 15697 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 181105 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 181105 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 122390 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 122390 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 126081 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 126081 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 136199 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 136199 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 206199 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 206199 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 182452 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 182452 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 182536 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 182536 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 194652 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 194652 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 205343 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 205343 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 122626 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 122626 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 62072 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 62072 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 125283 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 125283 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 108893 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 108893 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 64118 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 64118 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 76406 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 76406 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 120812 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 120812 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 156069 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 156069 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 156503 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 156503 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 82735 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 82735 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 164237 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 164237 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 87501 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 87501 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 91895 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 91895 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 76314 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 76314 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 157397 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 157397 0 None -58 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding methodDisplacement of 2-[125I]-Iodomelatonin from human MT1 receptor expressed in CHO cell membranes after 120 mins by filter binding method
ChEMBL 294 4 1 2 3.0 CC(=O)NCC1Cc2ccccc2N(Cc2ccccc2)C1 10.1021/acs.jmedchem.8b00359
1358 124 35 None -870 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm800974d
3976006 124 35 None -870 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm800974d
CHEMBL285718 124 35 None -870 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 10.1021/jm800974d
44424020 84938 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 84938 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 83981 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 83981 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 123112 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 123112 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 29608 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 29608 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 166504 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 166504 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 65758 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 65758 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 163943 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 163943 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 165580 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 165580 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 3851 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm040768k
7772 3851 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm040768k
CHEMBL189449 3851 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cellsBinding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm040768k
127041168 136081 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 136081 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 3851 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm048956y
7772 3851 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm048956y
CHEMBL189449 3851 3 None -14 2 Human 8.2 pKi = 8.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 10.1021/jm048956y
127041168 136081 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 136081 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 23373 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 23373 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 21175 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 21175 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 116210 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 116210 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 167888 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 167888 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 16601 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 16601 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 194027 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 194027 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 85309 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 85309 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 102495 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 102495 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 64212 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 64212 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 112833 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 112833 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 116870 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 116870 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 158264 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 158264 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 180804 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 180804 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 2355 67 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm980684+
1363 2355 67 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm980684+
CHEMBL286615 2355 67 None -18 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1021/jm980684+
44264706 202725 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 202725 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 203342 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 203342 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 108897 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 108897 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 87113 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 87113 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 15678 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 15678 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 77235 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 77235 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 155457 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 155457 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 203192 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 203192 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 203260 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 203260 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 166479 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 166479 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 4114 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 4114 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 4114 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 4114 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 113965 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 113965 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 162743 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 162743 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 113965 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 113965 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 162743 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 162743 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 15752 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 15752 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 122645 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 122645 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 206097 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 206097 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 84750 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 84750 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 76726 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 76726 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 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm800974d
5311198 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm800974d
CHEMBL274438 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm800974d
1359 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm048956y
5311198 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm048956y
CHEMBL274438 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cellsInhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm048956y
1359 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm980684+
5311198 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm980684+
CHEMBL274438 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assayBinding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm980684+
1359 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm401343c
5311198 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm401343c
CHEMBL274438 2139 20 None -125 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells
ChEMBL 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10.1021/jm401343c
10925526 111842 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 111842 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 118176 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 118176 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 113653 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 113653 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 137387 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 137387 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 81146 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 81146 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 159250 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 159250 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 181992 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 181992 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 206707 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 206707 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 82910 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 82910 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 206065 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 206065 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 26742 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 26742 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 165937 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 165937 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 166359 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 166359 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 157181 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 157181 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 205794 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 205794 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 97853 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 97853 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 150831 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 150831 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 123872 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 123872 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 203958 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 203958 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 77895 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 77895 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 191025 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 191025 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 15702 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 15702 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 110381 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 110381 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 110381 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 110381 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 141500 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 141500 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 110381 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 110381 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 144281 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 144281 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 15724 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 15724 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 206049 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 206049 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 137604 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 137604 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 120811 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 120811 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 209342 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 1437 65 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 1437 65 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 1437 65 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 1437 65 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 1437 65 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 140357 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 140357 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 138749 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 138749 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 137299 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 137299 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 137370 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 137370 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 64123 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 64123 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 15783 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 15783 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 16476 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 16476 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 92644 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 92644 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 206580 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 206580 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 4175 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 4175 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 3853 6 None -588 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1ccc(cc1)N(c1ccccc1)CCNC(=O)C 10.1021/jm700957j
7923 3853 6 None -588 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1ccc(cc1)N(c1ccccc1)CCNC(=O)C 10.1021/jm700957j
CHEMBL394676 3853 6 None -588 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cellsDisplacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells
ChEMBL 284 6 1 3 3.0 COc1ccc(cc1)N(c1ccccc1)CCNC(=O)C 10.1021/jm700957j
9859693 73777 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 73777 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 206406 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 206406 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 2355 67 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1016/j.ejmech.2007.01.005
1363 2355 67 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1016/j.ejmech.2007.01.005
CHEMBL286615 2355 67 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cellsDisplacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells
ChEMBL 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10.1016/j.ejmech.2007.01.005
10044270 188953 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 188953 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 193722 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 193722 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 156970 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 156970 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 16592 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 16592 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 104397 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 104397 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 193722 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 193722 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 106575 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 106575 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 76894 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 76894 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 76787 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 76787 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 15704 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 15704 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 111163 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 111163 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 146198 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 146198 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 19746 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 19746 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 206026 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 206026 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 106466 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 106466 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 15721 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 15721 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 3381 10 None -275 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 10.1016/j.bmc.2008.08.052
22133318 3381 10 None -275 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 10.1016/j.bmc.2008.08.052
CHEMBL490188 3381 10 None -275 2 Human 7.1 pKi = 7.1 Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cellsDisplacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells
ChEMBL 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 10.1016/j.bmc.2008.08.052
44579115 181253 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 181253 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 60437 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 60437 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 158077 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 158077 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 84749 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 84749 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 206555 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 206555 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 206555 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 206555 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 96723 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 96723 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 203819 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 203819 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 206144 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 206144 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 174945 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 174945 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 174945 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 174945 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 101030 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 101030 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 206568 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 206568 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 206568 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 206568 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 193073 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 193073 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 138163 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 138163 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 16324 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 16324 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 85991 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 85991 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 112062 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 112062 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 112062 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 112062 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 7989 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 7989 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 85058 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 85058 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 159216 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 159216 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 178814 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 178814 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 8214 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 8214 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 64005 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 64005 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 122616 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 122616 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 17073 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 17073 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 60440 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 60440 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 136100 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 136100 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 136291 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 136291 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 166238 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 166238 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 8577 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 8577 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 15723 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 15723 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 921 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 921 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 921 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 185485 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 185485 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 136291 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 136291 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 84899 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 84899 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 137515 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 137515 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 187566 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 187566 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 16685 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 16685 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 137213 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 137213 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 155872 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 155872 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 155872 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 1815 1 None -100 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10.1021/jm401343c
44208891 1815 1 None -100 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10.1021/jm401343c
CHEMBL3260983 1815 1 None -100 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cellsDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
ChEMBL 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10.1021/jm401343c
54582195 60438 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 60438 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 165587 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 165587 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 62074 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 62074 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 203523 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 203523 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 203733 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 203733 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 11225 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 11225 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 11225 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 82477 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 82477 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 60436 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 60436 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 148683 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 148683 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 203142 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 203142 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 203288 3 None -7 2 Human 7.0 pKi = 7 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 5 1 3 3.8 COc1cccc(Oc2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
CHEMBL7673 203288 3 None -7 2 Human 7.0 pKi = 7 Binding
Binding affinity towards human melatonin receptor type 1ABinding affinity towards human melatonin receptor type 1A
ChEMBL 283 5 1 3 3.8 COc1cccc(Oc2ccc(NC(=O)C3CC3)cc2)c1 10.1016/j.bmcl.2003.11.030
145979282 166122 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 166122 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
198 310 120 125I-Iodomelatonin -1 5 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 125I-Iodomelatonin -1 5 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 125I-Iodomelatonin -1 5 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 125I-Iodomelatonin -1 5 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 125I-Iodomelatonin -1 5 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 1819 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 1819 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 214329 0 35S-GTPGammaS - 1 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 330 9 0 8 2.1 CCOC(=O)CC(C(=O)OCC)SP(=S)(OC)OC None
1357 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
198 310 120 125I-Mel -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 125I-Mel -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 125I-Mel -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 125I-Mel -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 125I-Mel -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
198 310 120 125I-Iodomelatonin -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 125I-Iodomelatonin -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 125I-Iodomelatonin -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 125I-Iodomelatonin -1 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 125I-Iodomelatonin -1 5 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
198 310 120 None -1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
82148 310 120 None -1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
99 310 120 None -1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
CHEMBL10878 310 120 None -1 5 Human 8.0 pKi = 8.0 Binding
Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligandBinding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand
Drug Central 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 None
DB06594 310 120 None -1 5 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 3236 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
208902 3236 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
2355 3236 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
CHEMBL1218 3236 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
DB00980 3236 98 None 3 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 None
5 139 66 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-Mel -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 141 116 125I-Iodomelatonin -14791 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 125I-Iodomelatonin -14791 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 125I-Iodomelatonin -14791 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
4209 3114 71 125I-Mel -63095 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3114 71 125I-Mel -63095 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3114 71 125I-Mel -63095 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3114 71 125I-Mel -63095 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3114 71 125I-Mel -63095 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3114 71 125I-Mel -63095 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
1357 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2355 67 125I-Iodomelatonin -18 2 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1363 2355 67 125I-Iodomelatonin -18 2 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
CHEMBL286615 2355 67 125I-Iodomelatonin -18 2 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
70547 112844 72 125I-Iodomelatonin -10 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
CHEMBL33171 112844 72 125I-Iodomelatonin -10 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
1349 1819 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 1819 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 214332 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 112402 83 125I-Iodomelatonin 1 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
CHEMBL33103 112402 83 125I-Iodomelatonin 1 2 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
122162 2355 67 125I-Iodomelatonin -18 2 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1363 2355 67 125I-Iodomelatonin -18 2 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
CHEMBL286615 2355 67 125I-Iodomelatonin -18 2 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1357 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 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 2450 133 125I-Iodomelatonin -1 8 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1358 124 35 125I-Iodomelatonin -870 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 None
3976006 124 35 125I-Iodomelatonin -870 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 None
CHEMBL285718 124 35 125I-Iodomelatonin -870 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 None
None 214328 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 214328 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 1437 65 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 1437 65 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 1437 65 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 1437 65 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 1437 65 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 214333 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 2355 67 125I-Iodomelatonin -18 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1363 2355 67 125I-Iodomelatonin -18 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
CHEMBL286615 2355 67 125I-Iodomelatonin -18 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 None
1357 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 2450 133 125I-Mel -1 8 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 112402 83 125I-Iodomelatonin 1 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
CHEMBL33103 112402 83 125I-Iodomelatonin 1 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 3 3 2 1.6 CC(=O)NCCc1c[nH]c2ccc(O)cc12 None
70547 112844 72 125I-Iodomelatonin -10 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
CHEMBL33171 112844 72 125I-Iodomelatonin -10 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 202 3 2 1 1.8 CC(=O)NCCc1c[nH]c2ccccc12 None
10220503 3699 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 3699 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 3699 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 3699 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 3699 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 214328 0 125I-Mel -1 2 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 218 2 2 4 1.5 CC(=O)N1C=C(C2=C1C=CC(=C2)O)CCN None
198 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
198 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
82148 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
82148 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
99 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
99 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
CHEMBL10878 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
CHEMBL10878 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 9618428
DB06594 310 120 None -1 5 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 4 1 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)ccc2 12764576
DB06594 310 120 None -1 5 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 1503 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 1503 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 1503 1 None 6 2 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 273 4 1 4 1.5 CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 21568291
71533431 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 23265885
7775 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 23265885
CHEMBL2314259 78 0 None 2 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 1 3 3.0 COc1ccc2c(c1/C=C/NC(=O)C)cc(cc2)OC 23265885
57381112 1388 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 1388 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 1388 0 None 20 2 Human 10.5 pKi = 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 1 2 2.8 COc1ccc2c(c1)c(CCNC(=O)C(F)F)ccc2 22301214
115348 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
115348 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
1343 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
1343 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
CHEMBL289233 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
CHEMBL289233 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
DB08190 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 12764576
DB08190 70 42 None 4 2 Human 10.6 pKi = 10.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 358 4 2 2 2.5 COc1ccc2c(c1)c(CCNC(=O)C)c([nH]2)I 2991499
1356 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
208902 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
2355 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
CHEMBL1218 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
DB00980 3236 98 None 3 2 Human 10.9 pKi = 10.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 4 1 2 2.6 CCC(=O)NCC[C@@H]1CCc2c1c1CCOc1cc2 15695169
11196 1955 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 1955 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 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10696085
122162 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 12764576
122162 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 2843633
122162 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 9089668
1363 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10696085
1363 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 12764576
1363 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 2843633
1363 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 9089668
CHEMBL286615 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 10696085
CHEMBL286615 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 12764576
CHEMBL286615 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 2843633
CHEMBL286615 2355 67 None -18 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 5 2 1 3.4 CC(=O)NCCc1c(Cc2ccccc2)[nH]c2c1cccc2 9089668
7773 3852 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 3852 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 3851 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 15293992
11185529 3851 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 17907131
7772 3851 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 15293992
7772 3851 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 17907131
CHEMBL189449 3851 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 15293992
CHEMBL189449 3851 3 None -14 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 3 1 2 3.1 COc1ccc2c(c1)C(CNC(=O)C)Cc1c(C2)cccc1 17907131
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 12764576
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 2991499
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9089668
1346 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9618428
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 12764576
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 2991499
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9089668
1858 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9618428
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 12764576
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 2991499
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9089668
CHEMBL34730 160 42 None -25 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 4 2 2 2.5 COc1cc2c(CCNC(=O)C)c[nH]c2cc1Cl 9618428
24763223 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 22927210
8289 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 22927210
CHEMBL3260987 214 0 None 74 2 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 10 1 3 3.7 CC(=O)NCCN(c1cccc(c1)OCCCCc1ccccc1)C 22927210
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10696085
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 2991499
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9089668
1347 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9618428
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10696085
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 2991499
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9089668
1864 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9618428
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 10696085
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 2991499
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9089668
CHEMBL127421 162 51 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 4 3 3 1.6 COc1cc2c(CCNC(=O)C)c[nH]c2cc1O 9618428
24750192 3854 10 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 18052314
7777 3854 10 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 18052314
CHEMBL237236 3854 10 None -1 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 222 5 1 3 1.3 COc1cccc(c1)N(CCNC(=O)C)C 18052314
12324 3848 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 3848 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 3848 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 801 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 801 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 801 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 2450 133 None -1 8 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 3699 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 3699 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 3699 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 3699 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 3699 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 214329 0 None - 1 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 330 9 0 8 2.1 CCOC(=O)CC(C(=O)OCC)SP(=S)(OC)OC None
1351 2363 15 None -1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 15302228
219018 2363 15 None -1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 15302228
CHEMBL4079759 2363 15 None -1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 280 4 2 2 3.1 COc1cc2c(cc1Cl)[nH]cc2[C@H](CNC(=O)C)C 15302228
127856 3378 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 3378 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 3378 0 None -3 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 253 4 1 1 3.3 O=C(C1CCC1)NCCc1cccc2c1cccc2 12764576
1358 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 12764576
1358 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9089668
1358 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9737724
3976006 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 12764576
3976006 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9089668
3976006 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9737724
CHEMBL285718 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 12764576
CHEMBL285718 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9089668
CHEMBL285718 124 35 None -870 2 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 3 1 1 3.7 CCC(=O)NC1Cc2ccccc2C(C1)c1ccccc1 9737724
1348 1815 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10205014
1348 1815 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 9089668
44208891 1815 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10205014
44208891 1815 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 9089668
CHEMBL3260983 1815 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 10205014
CHEMBL3260983 1815 1 None -100 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 2 1 2 2.9 COc1ccc2c(c1)c(c[nH]2)C1CCCN(C1)C(=O)C 9089668
1354 3381 10 None -275 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 12764576
22133318 3381 10 None -275 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 12764576
CHEMBL490188 3381 10 None -275 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 5 2 3 3.8 COc1ccc2c(c1)c(CCNC(=O)C)cc(c2)c1cccc(c1)N 12764576
1359 2139 20 None -125 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10737738
5311198 2139 20 None -125 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10737738
CHEMBL274438 2139 20 None -125 2 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 376 6 1 3 4.7 CCCC(=O)NCCc1c2c3ccccc3CCCn2c2c1cc(OC)cc2 10737738
1353 3380 3 None -112 2 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 12764576
9998187 3380 3 None -112 2 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 12764576
CHEMBL33549 3380 3 None -112 2 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 7 1 4 3.7 COc1cccc(c1)Cc1oc2c(c1CCNC(=O)C)cc(cc2)OC 12764576
10849065 137 8 None 4 2 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 11068946
1345 137 8 None 4 2 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 11068946
CHEMBL126809 137 8 None 4 2 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 6 3 3 1.2 OCCOc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 11068946
1361 3379 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 3379 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 1959 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 1959 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 1959 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 3382 18 None 39 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
9870523 3382 18 None 39 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
CHEMBL429392 3382 18 None 39 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 12 2 4 5.2 CC(=O)NCCc1cccc2c1cc(OCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
1355 3383 3 None 70 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
9806449 3383 3 None 70 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
CHEMBL14453 3383 3 None 70 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 512 13 2 4 5.6 CC(=O)NCCc1cccc2c1cc(OCCCCOc1ccc3c(c1)c(CCNC(=O)C)ccc3)cc2 12764576
1349 1819 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 1819 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 1819 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 1819 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