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ChEMBL ligand: CHEMBL2413367 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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OX1 receptor/Orexin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613] | ||||||||
ChEMBL | Binding affinity to human OXIR | B | 8.22 | pKi | 6 | nM | Ki | ACS Med Chem Lett (2020) 11: 2002-2009 [PMID:33062185] |
ChEMBL | Binding affinity to orexin receptor 1 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
ChEMBL | Antagonist activity at OX1 receptor (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2013) 56: 6901-6916 [PMID:23941044] |
ChEMBL | Antagonist activity at orexin-1 receptor (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2875-2887 [PMID:26045032] |
OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614] | ||||||||
ChEMBL | Displacement of (2S)-N-(2-pyrrol-1-ylphenyl)-1-[2-[1-(tritritiomethyl)benzimidazol-2-yl]sulfanylacetyl]pyrrolidine-2-carboxamide from human OX2 receptor expressed on CHO cell membrane measured after 3 hrs by TopCount method | B | 6.38 | pKi | 417 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 5809-5814 [PMID:27818110] |
ChEMBL | Binding affinity to human OX2R | B | 6.38 | pKi | 417 | nM | Ki | ACS Med Chem Lett (2020) 11: 2002-2009 [PMID:33062185] |
ChEMBL | Binding affinity to orexin receptor 2 (unknown origin) | B | 6.38 | pIC50 | 417 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
ChEMBL | Antagonist activity at OX2 receptor (unknown origin) | B | 6.38 | pIC50 | 417 | nM | IC50 | J Med Chem (2013) 56: 6901-6916 [PMID:23941044] |
ChEMBL | Antagonist activity at orexin-2 receptor (unknown origin) | B | 6.38 | pIC50 | 417 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2875-2887 [PMID:26045032] |
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]