CIFEA [Ligand Id: 7780] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1774519 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] | ||||||||
| ChEMBL | Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting | B | 8.04 | pKi | 9.2 | nM | Ki | J Med Chem (2011) 54: 3436-3444 [PMID:21473625] |
| ChEMBL | 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 Readers | F | 8.35 | pEC50 | 4.47 | nM | EC50 | J Med Chem (2011) 54: 3436-3444 [PMID:21473625] |
| MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] | ||||||||
| GtoPdb | - | - | 10.9 | pKi | - | - | - | J Med Chem (2011) 54: 3436-44 [PMID:21473625] |
| ChEMBL | Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting | B | 10.92 | pKi | 0.01 | nM | Ki | J Med Chem (2011) 54: 3436-3444 [PMID:21473625] |
| ChEMBL | Agonist activity at human MT2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers | F | 8.88 | pEC50 | 1.32 | nM | EC50 | J Med Chem (2011) 54: 3436-3444 [PMID:21473625] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
