AAE-M-PBP-amine [Ligand Id: 8289] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3260987
  • 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 - - 8.9 pKi - - - ChemMedChem (2012) 7: 1954-64 [PMID:22927210]
ChEMBL Agonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation F 8.93 pKi 1.17 nM Ki J. Med. Chem. (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in rat NIH3T3 cells after 90 mins B 8.93 pKi 1.17 nM Ki MedChemComm (2015) 6: 1340-1344
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
ChEMBL Agonist activity at MT2 receptor (unknown origin) expressed in mouse NIH3T3 cells assessed as inhibition of forskolin-induced cAMP accumulation F 7.04 pKi 91.2 nM Ki J. Med. Chem. (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in rat NIH3T3 cells after 90 mins B 7.04 pKi 91 nM Ki MedChemComm (2015) 6: 1340-1344

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]