daridorexant [Ligand Id: 11648] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4297590 (Act-541468, ACT-541468, Daridorexant, DEA NO. 2410, Nemorexant)
  • OX1 receptor/Orexin receptor 1 in Human [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613]
  • OX1 receptor in Dog [GtoPdb: 321]
  • OX1 receptor in Rat [GtoPdb: 321] [UniProtKB: P56718]
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  • OX2 receptor/Orexin receptor 2 in Human [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614]
  • OX2 receptor in Dog [GtoPdb: 322]
  • OX2 receptor in Rat [GtoPdb: 322] [UniProtKB: P56719]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
OX1 receptor/Orexin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613]
ChEMBL Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX1 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liquid scintillation counting method B 8.8 pKi 1.58 nM Ki J Med Chem (2020) 63: 1528-1543 [PMID:31860301]
GtoPdb - - 8.8 pKi 1.58 nM Ki J Med Chem (2020) 63: 1528-1543 [PMID:31860301]
OX1 receptor in Dog [GtoPdb: 321]
OX1 receptor in Rat [GtoPdb: 321] [UniProtKB: P56718]
OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614]
ChEMBL Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX2 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liquid scintillation counting method B 8.9 pKi 1.26 nM Ki J Med Chem (2020) 63: 1528-1543 [PMID:31860301]
OX2 receptor in Dog [GtoPdb: 322]
OX2 receptor in Rat [GtoPdb: 322] [UniProtKB: P56719]

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]