Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 57781216 | 125914 | None | 1 | Human | Functional | pEC50 | = | 10.8 | 10.8 | 8 | 2 | 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 | 125914 | None | 1 | Human | Functional | pEC50 | = | 10.8 | 10.8 | 8 | 2 | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay |
ChEMBL | 258 | 3 | 1 | 3 | 2.7 | CC(=O)NCC[C@@H]1CCc2ccc3nc(C)oc3c21 | 10.1021/acs.jmedchem.0c01836 | ||
| 24954989 | 1532 | None | 1 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 25 | 2 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 273 | 4 | 1 | 4 | 1.5 | CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 | 10.1021/jm200385u | ||
| 7774 | 1532 | None | 1 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 25 | 2 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 273 | 4 | 1 | 4 | 1.5 | CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 | 10.1021/jm200385u | ||
| CHEMBL1802025 | 1532 | None | 1 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 25 | 2 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 273 | 4 | 1 | 4 | 1.5 | CCc1nn2c(c1CCNC(=O)C)c1CCOc1cc2 | 10.1021/jm200385u | ||
| 1357 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 1 | 5 | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.0c01836 | ||
| 1672 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 1 | 5 | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.0c01836 | ||
| 224 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 1 | 5 | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.0c01836 | ||
| 896 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 1 | 5 | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.0c01836 | ||
| CHEMBL45 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 1 | 5 | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.0c01836 | ||
| DB01065 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.7 | 10.7 | 1 | 5 | Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assayAgonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.0c01836 | ||
| 1357 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200221q | ||
| 1672 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200221q | ||
| 224 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200221q | ||
| 896 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200221q | ||
| CHEMBL45 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200221q | ||
| DB01065 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate ReadersAgonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200221q | ||
| 1357 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200385u | ||
| 1672 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200385u | ||
| 224 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200385u | ||
| 896 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200385u | ||
| CHEMBL45 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate readerAgonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm200385u | ||
| DB01065 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.6 | 10.6 | 1 | 5 | 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 | 184937 | None | 0 | Human | Functional | pEC50 | = | 10.5 | 10.5 | 3 | 2 | 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 | 184937 | None | 0 | Human | Functional | pEC50 | = | 10.5 | 10.5 | 3 | 2 | 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 | 184703 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 4 | 2 | 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 | 184703 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 4 | 2 | 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 | 184964 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | -2 | 2 | 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 | 184964 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | -2 | 2 | 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 | 185435 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 2 | 2 | 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 | 185435 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 2 | 2 | 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 | 185110 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 5 | 2 | 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 | 185110 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | 5 | 2 | 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 | 186373 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | -2 | 2 | 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 | 186373 | None | 0 | Human | Functional | pEC50 | = | 10.4 | 10.4 | -2 | 2 | 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 | 166762 | None | 0 | Human | Functional | pEC50 | = | 10.3 | 10.3 | - | 1 | 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 | 166762 | None | 0 | Human | Functional | pEC50 | = | 10.3 | 10.3 | - | 1 | 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 | 185402 | None | 19 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 6 | 2 | 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 | 185402 | None | 19 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 6 | 2 | Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assayAgonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay |
ChEMBL | 297 | 5 | 1 | 5 | 1.8 | COc1cc2c(cc1Cl)nc(OC)n2CCNC(C)=O | 10.1021/acs.jmedchem.0c00627 | ||
| 1357 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assayAgonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.ejmech.2023.115152 | ||
| 1672 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assayAgonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.ejmech.2023.115152 | ||
| 224 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assayAgonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.ejmech.2023.115152 | ||
| 896 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assayAgonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.ejmech.2023.115152 | ||
| CHEMBL45 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assayAgonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.ejmech.2023.115152 | ||
| DB01065 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assayAgonist activity at human melatonin MT1 receptor expressed in HEK293 cells co-transfected with Galphai9 chimera construct assessed as stimulation of inositol phosphate production by HTRF based assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.ejmech.2023.115152 | ||
| 1357 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.2c00717 | ||
| 1672 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.2c00717 | ||
| 224 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.2c00717 | ||
| 896 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assayAgonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/acs.jmedchem.2c00717 | ||
| CHEMBL45 | 2485 | None | 75 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 1 | 5 | 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 | ||
Showing 1 to 50 of 473 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 10440 | 2680 | None | 22 | Human | Binding | pEC50 | = | 6.5 | 6.5 | -21 | 3 | Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay |
ChEMBL | 417 | 7 | 3 | 7 | 4.2 | OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F | 10.1021/acs.jmedchem.9b00869 | ||
| 139030523 | 2680 | None | 22 | Human | Binding | pEC50 | = | 6.5 | 6.5 | -21 | 3 | Agonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assayAgonist activity at human MT1 receptor expressed in HTLA cells assessed as stimulation of beta-arrestin recruitment incubated for 16 to 20 hrs by bright-glo luminescence assay |
ChEMBL | 417 | 7 | 3 | 7 | 4.2 | OCc1cccc(c1c1nc(NCc2ccc(cc2)Oc2ccccc2)nc(n1)N)F | 10.1021/acs.jmedchem.9b00869 | ||
| CHEMBL4449712 | 2680 | None | 22 | Human | Binding | pEC50 | = | 6.5 | 6.5 | -21 | 3 | 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 | 121392 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | -8 | 2 | 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 | 121392 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | -8 | 2 | 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 | 30974 | None | 0 | Human | Binding | pIC50 | = | 10.9 | 10.9 | - | 0 | Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin 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 | 30974 | None | 0 | Human | Binding | pIC50 | = | 10.9 | 10.9 | - | 0 | Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin 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 | 112385 | None | 0 | Human | Binding | pIC50 | = | 10.8 | 10.8 | -25 | 2 | Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin 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 | 112385 | None | 0 | Human | Binding | pIC50 | = | 10.8 | 10.8 | -25 | 2 | Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin 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 | 125919 | None | 0 | Human | Binding | pIC50 | = | 10.7 | 10.7 | - | 0 | 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 | 125919 | None | 0 | Human | Binding | pIC50 | = | 10.7 | 10.7 | - | 0 | 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 | 125917 | None | 0 | Human | Binding | pIC50 | = | 10.5 | 10.5 | - | 0 | 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 | 125917 | None | 0 | Human | Binding | pIC50 | = | 10.5 | 10.5 | - | 0 | 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 | 125921 | None | 0 | Human | Binding | pIC50 | = | 10.4 | 10.4 | - | 0 | 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 | 125921 | None | 0 | Human | Binding | pIC50 | = | 10.4 | 10.4 | - | 0 | 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 | 125914 | None | 1 | Human | Binding | pIC50 | = | 10.2 | 10.2 | 2 | 2 | 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 | 125914 | None | 1 | Human | Binding | pIC50 | = | 10.2 | 10.2 | 2 | 2 | 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 | 125911 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 0 | 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 | 125911 | None | 0 | Human | Binding | pIC50 | = | 10.2 | 10.2 | - | 0 | 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 | 160930 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | 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 | 160930 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | 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 | 125927 | None | 0 | Human | Binding | pIC50 | = | 10.0 | 10.0 | - | 0 | 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 | 125927 | None | 0 | Human | Binding | pIC50 | = | 10.0 | 10.0 | - | 0 | Binding Assay: Binding assay using melatonin receptors 1 or 2.Binding Assay: Binding assay using melatonin receptors 1 or 2. |
ChEMBL | 312 | 3 | 1 | 3 | 3.2 | Cc1nc2ccc3c(c2o1)C(CCNC(=O)C(F)(F)F)CC3 | nan | ||
| 1357 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.03.006 | ||
| 1672 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.03.006 | ||
| 224 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.03.006 | ||
| 896 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.03.006 | ||
| CHEMBL45 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.03.006 | ||
| DB01065 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cellsDisplacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.03.006 | ||
| 1357 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.11.014 | ||
| 1672 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.11.014 | ||
| 224 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.11.014 | ||
| 896 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.11.014 | ||
| CHEMBL45 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1016/j.bmc.2016.11.014 | ||
| DB01065 | 2485 | None | 75 | Human | Binding | pIC50 | = | 10.0 | 10.0 | -1 | 8 | 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 | 125916 | None | 0 | Human | Binding | pIC50 | = | 9.9 | 9.9 | 1 | 2 | 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 | 125916 | None | 0 | Human | Binding | pIC50 | = | 9.9 | 9.9 | 1 | 2 | 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 | 125913 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | 1 | 2 | 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 | 125913 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | 1 | 2 | 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 | 125920 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | 2 | 2 | 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 | 125920 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | 2 | 2 | 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 | 9776 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin 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 | 9776 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin 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 | 161661 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | 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 | 161661 | None | 0 | Human | Binding | pIC50 | = | 9.8 | 9.8 | - | 0 | Displacement of [125I]NDP-alpha -MSH from human recombinant MT1 receptor after 240 mins by scintillation counting analysisDisplacement of [125I]NDP-alpha -MSH from human recombinant MT1 receptor after 240 mins by scintillation counting analysis |
ChEMBL | 583 | 8 | 3 | 6 | 5.8 | CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 | 10.1016/j.bmcl.2018.03.093 | ||
| 1357 | 2485 | None | 75 | Human | Binding | pIC50 | = | 9.7 | 9.7 | -1 | 8 | Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm8007618 | ||
| 1672 | 2485 | None | 75 | Human | Binding | pIC50 | = | 9.7 | 9.7 | -1 | 8 | Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm8007618 | ||
| 224 | 2485 | None | 75 | Human | Binding | pIC50 | = | 9.7 | 9.7 | -1 | 8 | Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm8007618 | ||
| 896 | 2485 | None | 75 | Human | Binding | pIC50 | = | 9.7 | 9.7 | -1 | 8 | Displacement of radiolabeled melatonin from human MT1 receptorDisplacement of radiolabeled melatonin from human MT1 receptor |
ChEMBL | 232 | 4 | 2 | 2 | 1.9 | COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 | 10.1021/jm8007618 | ||
| CHEMBL45 | 2485 | None | 75 | Human | Binding | pIC50 | = | 9.7 | 9.7 | -1 | 8 | 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 | ||
Showing 1 to 50 of 3,385 entries