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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL189449
  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
There should be some charts here, you may need to enable JavaScript!
  • MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
There should be some charts here, you may need to enable JavaScript!
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 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]