TCS 1102 [Ligand Id: 9304] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL429848
  • OX1 receptor/Orexin receptor 1 in Human [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613]
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  • OX2 receptor/Orexin receptor 2 in Human [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614]
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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]
GtoPdb - - 8.52 pKi 3 nM Ki Bioorg Med Chem Lett (2008) 18: 1425-30 [PMID:18207395]
ChEMBL Displacement of [3H](S)-1-[2-(1-methyl-1H-benzoimidazol-2-ylsulfanyl)-acetyl]-pyrrolidine-2-carboxylic acid biphenyl-2-ylamide from human OX1R expressed in CHO cells B 8.52 pKi 3 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 1425-1430 [PMID:18207395]
OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614]
ChEMBL Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R expressed in CHO cells B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 1425-1430 [PMID:18207395]
ChEMBL Displacement of [125I]-orexin A from human OX2 receptor expressed in CHO cell membranes after 90 mins by scintillation counting B 9.7 pKi 0.2 nM Ki J Med Chem (2016) 59: 8263-8275 [PMID:27546834]
GtoPdb - - 9.7 pKi 0.2 nM Ki Bioorg Med Chem Lett (2008) 18: 1425-30 [PMID:18207395]

ChEMBL data shown on this page come from version 28:

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