S24014 [Ligand Id: 1353] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL33549
  • 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 Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells B 7.39 pKi 40.74 nM Ki J Med Chem (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Binding affinity on human melatonin receptor type 1A stably transfected in human embryonic kidney (HEK 293) using 2-[125I]iodomelatonin as radioligand. B 7.39 pKi 40.6 nM Ki J Med Chem (2002) 45: 2788-2800 [PMID:12061881]
ChEMBL Displacement of [125I]2-iodomelatonin from MT1 receptor (unknown origin) expressed in HEK293 cells B 7.39 pKi 40.6 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
GtoPdb - - 7.5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells B 7.57 pKi 27 nM Ki J Med Chem (2009) 52: 826-833 [PMID:19193160]
ChEMBL Intrinsic activity evaluated on [35S]GTP -gamma-S binding in Chinese hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A F 7.43 pEC50 37 nM EC50 J Med Chem (2002) 45: 2788-2800 [PMID:12061881]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
ChEMBL Displacement of [125I]2-iodomelatonin from MT2 receptor (unknown origin) expressed in HEK293 cells B 9.48 pKi 0.33 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells B 9.49 pKi 0.32 nM Ki J Med Chem (2005) 48: 4049-4060 [PMID:15943478]
ChEMBL Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]iodomelatonin as radioligand. B 9.49 pKi 0.32 nM Ki J Med Chem (2002) 45: 2788-2800 [PMID:12061881]
GtoPdb - - 9.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2003) 367: 553-61 [PMID:12764576]
ChEMBL Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells B 9.6 pKi 0.25 nM Ki J Med Chem (2009) 52: 826-833 [PMID:19193160]
ChEMBL Intrinsic activity at human Melatonin receptor type 1B evaluated on [35S]GTP-gamma-S, binding in Chinese hamster ovarian (CHO) cells F 9.14 pEC50 0.72 nM EC50 J Med Chem (2002) 45: 2788-2800 [PMID:12061881]

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]