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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]