UCM 549 [Ligand Id: 7772] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL189449
  • 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 Antagonist activity at MT1 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay F 7.57 pKi 27 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
GtoPdb - - 8.2 pKi - - - J Med Chem (2004) 47: 4202-12 [PMID:15293992];
ChemMedChem (2007) 2: 1741-9 [PMID:17907131]
ChEMBL Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells B 8.21 pKi 6.17 nM Ki J Med Chem (2004) 47: 4202-4212 [PMID:15293992]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells B 8.21 pKi 6.17 nM Ki J Med Chem (2005) 48: 4049-4060 [PMID:15943478]
MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
ChEMBL Antagonist activity at MT2 receptor (unknown origin) expressed in mouse NIH3T3 cells by [35S]GTPgammaS binding assay F 8.89 pKi 1.3 nM Ki J Med Chem (2014) 57: 3161-3185 [PMID:24228714]
ChEMBL Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells B 9.18 pKi 0.66 nM Ki J Med Chem (2004) 47: 4202-4212 [PMID:15293992]
ChEMBL Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells B 9.18 pKi 0.66 nM Ki J Med Chem (2005) 48: 4049-4060 [PMID:15943478]
GtoPdb - - 9.2 pKi - - - J Med Chem (2004) 47: 4202-12 [PMID:15293992];
ChemMedChem (2007) 2: 1741-9 [PMID:17907131]

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]