compound 11 [PMID: 15261275] [Ligand Id: 9415] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL185088
  • 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 Radioligand displacement assay using [125I]-orexin A as radio ligand. - 5.3 pKi >5012 nM Ki Bioorg Med Chem Lett (2004) 14: 4225-9 [PMID:15261275]
ChEMBL Binding affinity towards human orexin receptor type 1 was determined using [125I]-Orexin A as radio ligand B 5.3 pKi <5011.87 nM Ki Bioorg Med Chem Lett (2004) 14: 4225-4229 [PMID:15261275]
ChEMBL Binding affinity to OX1 receptor B 8.2 pKi 6.31 nM Ki J Med Chem (2009) 52: 891-903 [PMID:19199652]
OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614]
ChEMBL Binding affinity to OX2 receptor B 5.3 pKi >5011.87 nM Ki J Med Chem (2009) 52: 891-903 [PMID:19199652]
ChEMBL Binding affinity towards human orexin receptor type 2 was determined using [125I]-Orexin A as radio ligand B 8.2 pKi 6.31 nM Ki Bioorg Med Chem Lett (2004) 14: 4225-4229 [PMID:15261275]
GtoPdb Radioligand displacement assay using [125I]-orexin A as radio ligand. - 8.3 pKi 5.01 nM Ki Bioorg Med Chem Lett (2004) 14: 4225-9 [PMID:15261275]

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]