tasimelteon [Ligand Id: 7393] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2103822 (BMS-214778, BMS-214,778, Hetlioz, Hetlioz lq, Tasimelteon, VEC-162)
  • MT1 receptor in Human [GtoPdb: 287] [UniProtKB: P48039]
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  • MT2 receptor in Human [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 in Human [GtoPdb: 287] [UniProtKB: P48039]
GtoPdb - - 9.5 pKi 0.3 nM Ki Tasimelteon Advisory Committee Meeting Briefing Materials.. FDA;
Lancet (2009) 373: 482-91 [PMID:19054552]
MT2 receptor in Human [GtoPdb: 288] [UniProtKB: P49286]
GtoPdb - - 10.2 pKi 0.07 nM Ki Tasimelteon Advisory Committee Meeting Briefing Materials.. FDA;
Lancet (2009) 373: 482-91 [PMID:19054552]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]