K185 [Ligand Id: 1359] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL274438
  • 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]
ChEMBL Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 7.18 pKi 66.1 nM Ki J. Med. Chem. (2000) 43: 1050-1061 [PMID:10737738]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in mouse NIH3T3 cells B 7.18 pKi 66.1 nM Ki J. Med. Chem. (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells B 7.18 pKi 66.07 nM Ki J. Med. Chem. (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 7.18 pKi 66 nM Ki J. Med. Chem. (2009) 52: 826-833 [PMID:19193160]
GtoPdb - - 7.2 pKi - - - J Med Chem (2000) 43: 1050-61 [PMID:10737738]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
GtoPdb - - 9.29 pKi 0.51 nM Ki J Med Chem (2000) 43: 1050-61 [PMID:10737738];
Reprod Nutr Dev (1999) 39: 335-44 [PMID:10420436]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2000) 43: 1050-1061 [PMID:10737738]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2009) 52: 826-833 [PMID:19193160]
ChEMBL Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in mouse NIH3T3 cells B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2014) 57: 3161-3185 [PMID:24228714]

ChEMBL data shown on this page come from version 28:

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]