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

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ChEMBL ligand: CHEMBL2103822 (BMS-214,778, BMS-214778, 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 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]