MK-1064 [Ligand Id: 9306] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL3338866 (Mk-1064, MK 1064) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 | - | - | 5.8 | pKi | 1584 | nM | Ki | ChemMedChem (2014) 9: 311-22 [PMID:24376006] |
| ChEMBL | Binding affinity to human OX1 receptor expressed in CHO cell membranes by scintillation counting analysis | B | 5.8 | pKi | 1584 | nM | Ki | J Med Chem (2015) 58: 5620-5636 [PMID:26087021] |
| ChEMBL | Binding affinity to human orexin-1 receptor expressed in CHO cell membranes after 3 hrs by radioligand displacement assay | B | 5.8 | pKi | 1584 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 2875-2887 [PMID:26045032] |
| ChEMBL | Antagonist activity at human OX1R expressed in CHO cells by FLIPR assay | B | 5.75 | pIC50 | 1789 | nM | IC50 | J Med Chem (2016) 59: 504-530 [PMID:26317591] |
| OX1 receptor in Dog [GtoPdb: 321] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - |
ChemMedChem (2014) 9: 311-22 [PMID:24376006]; Sci Rep (2022) 12: 8473 [PMID:35589803] |
| OX1 receptor in Mouse [GtoPdb: 321] [UniProtKB: P58307] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - |
ChemMedChem (2014) 9: 311-22 [PMID:24376006]; Sci Rep (2022) 12: 8473 [PMID:35589803] |
| OX1 receptor in Rat [GtoPdb: 321] [UniProtKB: P56718] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - |
ChemMedChem (2014) 9: 311-22 [PMID:24376006]; Sci Rep (2022) 12: 8473 [PMID:35589803] |
| OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614] | ||||||||
| GtoPdb | - | - | 9.3 | pKi | 0.5 | nM | Ki | ChemMedChem (2014) 9: 311-22 [PMID:24376006] |
| ChEMBL | Displacement of (S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-((3H)-1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting analysis | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2015) 58: 5620-5636 [PMID:26087021] |
| ChEMBL | Displacement of (S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1[3H]-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human orexin-2 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting analysis | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 2875-2887 [PMID:26045032] |
| ChEMBL | Antagonist activity at human OX2R expressed in CHO cells by FLIPR assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2016) 59: 504-530 [PMID:26317591] |
| OX2 receptor in Dog [GtoPdb: 322] | ||||||||
| GtoPdb | - | - | 9.1 | pKi | - | - | - |
ChemMedChem (2014) 9: 311-22 [PMID:24376006]; Sci Rep (2022) 12: 8473 [PMID:35589803] |
| OX2 receptor in Mouse [GtoPdb: 322] [UniProtKB: P58308, P58308-2] | ||||||||
| GtoPdb | - | - | 9 | pKi | - | - | - |
ChemMedChem (2014) 9: 311-22 [PMID:24376006]; Sci Rep (2022) 12: 8473 [PMID:35589803] |
| OX2 receptor in Rat [GtoPdb: 322] [UniProtKB: P56719] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
ChemMedChem (2014) 9: 311-22 [PMID:24376006]; Sci Rep (2022) 12: 8473 [PMID:35589803] |
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]
