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 | Antagonist activity at OX1R (unknown origin) assessed as inhibition constant | B | 5.5 | pKi | 3162.28 | nM | Ki | J Med Chem (2021) 64: 9786-9874 [PMID:34213340] |
| 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] |
| ChEMBL | Antagonist activity at OX2R (unknown origin) assessed as inhibition constant | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2021) 64: 9786-9874 [PMID:34213340] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | 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]
