TCS-OX2-29 [Ligand Id: 4038] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL142009 |
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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] |
| ChEMBL | Antagonist activity at human OX1R | F | 5 | pIC50 | >10000 | nM | IC50 | RSC Med Chem (2024) 15: 344-354 [PMID:38283232] |
| 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 | Antagonist activity at human OX2R | F | 7.4 | pIC50 | 40 | nM | IC50 | RSC Med Chem (2024) 15: 344-354 [PMID:38283232] |
ChEMBL data shown on this page come from version 35:
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]
