TCS-OX2-29 [Ligand Id: 4038] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL142009
  • 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]
ChEMBL Inhibitory concentration against human orexin-1 receptor (hOX1R) B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 4497-4499 [PMID:14643355]
ChEMBL Antagonist activity at human OX1 receptor F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2009) 52: 891-903 [PMID:19199652]
ChEMBL Binding affinity to orexin receptor 1 (unknown origin) B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4761-4769 [PMID:23891187]
OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614]
GtoPdb - - 7.5 pKi - - - Bioorg Med Chem Lett (2003) 13: 4497-9 [PMID:14643355];
Br J Pharmacol (2014) 171: 351-63 [PMID:23692283]
ChEMBL Inhibitory concentration against human orexin-2 receptor (hOX2R) B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 4497-4499 [PMID:14643355]
ChEMBL Antagonist activity at human OX2 receptor F 7.4 pIC50 40 nM IC50 J. Med. Chem. (2009) 52: 891-903 [PMID:19199652]
ChEMBL Binding affinity to orexin receptor 2 (unknown origin) B 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4761-4769 [PMID:23891187]

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, 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]