JNJ-10397049 [Ligand Id: 1701] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL359632 (JNJ-10397049) |
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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 | Binding affinity towards human orexin receptor type 1 was determined using [125I]-Orexin A as radio ligand | B | 5.5 | pKi | 3162.28 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4225-4229 [PMID:15261275] |
| ChEMBL | Displacement of [125I]-orexin A from OX1 receptor (unknown origin) expressed in CHOK1 cells after 90 to 120 mins by scintillation counting analysis | B | 5.5 | pKi | 3162.28 | nM | Ki | J Med Chem (2015) 58: 5620-5636 [PMID:26087021] |
| ChEMBL | Binding affinity to orexin receptor 1 (unknown origin) | B | 5.78 | pKi | 1644 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Bioorg Med Chem Lett (2004) 14: 4225-9 [PMID:15261275] |
| ChEMBL | Displacement of [3H]-SB67404 from human orexin 1 receptor expressed in CHO cells incubated for 2 hrs by whole cell radioligand binding assay | B | 5.87 | pKi | 1348.96 | nM | Ki | J Med Chem (2020) 63: 11045-11053 [PMID:32977721] |
| ChEMBL | Binding affinity to OX1 receptor | B | 8.3 | pKi | 5.01 | 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 | 5.5 | pKi | 3162.28 | nM | Ki | J Med Chem (2009) 52: 891-903 [PMID:19199652] |
| ChEMBL | Binding affinity to orexin receptor 2 (unknown origin) | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
| ChEMBL | Binding affinity towards human orexin receptor type 2 was determined using [125I]-Orexin A as radio ligand | B | 8.3 | pKi | 5.01 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4225-4229 [PMID:15261275] |
| ChEMBL | Displacement of [125I]-orexin A from OX2 receptor (unknown origin) expressed in CHOK1 cells after 90 to 120 mins by scintillation counting analysis | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2015) 58: 5620-5636 [PMID:26087021] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | Bioorg Med Chem Lett (2004) 14: 4225-9 [PMID:15261275] |
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]
