EFPPEA [Ligand Id: 7774] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1802025
  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
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  • MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
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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]
GtoPdb - - 10.2 pKi 0.06 nM Ki J. Med. Chem. (2011) 54: 4207-18 [PMID:21568291]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 10.21 pKi 0.06 nM Ki J. Med. Chem. (2011) 54: 4207-4218 [PMID:21568291]
ChEMBL Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader F 10.68 pEC50 0.02 nM EC50 J. Med. Chem. (2011) 54: 4207-4218 [PMID:21568291]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.38 pKi 0.42 nM Ki J. Med. Chem. (2011) 54: 4207-4218 [PMID:21568291]
GtoPdb - - 9.4 pKi - - - J. Med. Chem. (2011) 54: 4207-18 [PMID:21568291]
ChEMBL Agonist activity at human MT2 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader F 9.28 pEC50 0.53 nM EC50 J. Med. Chem. (2011) 54: 4207-4218 [PMID:21568291]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]