S26131 [Ligand Id: 1362] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL429392
  • 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 Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis B 6.95 pKi 112.2 nM Ki Medchemcomm (2015) 6: 1340-1344
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis B 6.95 pKi 112 nM Ki Medchemcomm (2015) 6: 1340-1344
ChEMBL Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells B 8.41 pKi 3.9 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
GtoPdb - - 9.3 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]
ChEMBL Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand B 9.3 pKi 0.5 nM Ki J Med Chem (2003) 46: 1127-1129 [PMID:12646022]
ChEMBL Binding affinity to MT1 receptor (unknown origin) expressed in HEK cells B 9.3 pKi 0.5 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in HEK293 cells after 120 mins B 9.3 pKi 0.5 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 Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis B 6.45 pKi 354.81 nM Ki Medchemcomm (2015) 6: 1340-1344
ChEMBL Displacement of [125I]2-iodomelatonin from human MT2 receptor expressed in CHO cells B 6.83 pKi 149 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand B 6.95 pKi 112 nM Ki J Med Chem (2003) 46: 1127-1129 [PMID:12646022]
ChEMBL Binding affinity to MT2 receptor (unknown origin) expressed in HEK cells B 6.95 pKi 112 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in HEK293 cells after 120 mins B 6.95 pKi 112 nM Ki Medchemcomm (2015) 6: 1340-1344
GtoPdb - - 7 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]

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]