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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
