PF-05105679 [Ligand Id: 10300] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3577885 (Pf-05105679, PF 5105679) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of dofetilide binding to human ERG | B | 4.8 | pKi | >15857 | nM | Ki | ACS Med Chem Lett (2015) 6: 419-424 [PMID:25893043] |
| Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of GABA/PBR | B | 5.99 | pKi | 1023.29 | nM | Ki | Data for DCP probe PF-05105679 |
| ChEMBL | GPCRScan assay: inhibition of GABA/PBR | B | 5.99 | pKi | 1022.12 | nM | Ki | Data for DCP probe PF-05105679 |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Cold activation | B | 6.32 | pIC50 | 480 | nM | IC50 | Data for DCP probe PF-05105679 |
| ChEMBL | WS-12 ((2S,5R)-2-isopropyl-N-(4-methoxyphenyl)-5-methylcyclohexanecarboximide) agonist activation | B | 6.74 | pIC50 | 181 | nM | IC50 | Data for DCP probe PF-05105679 |
| ChEMBL | Antagonist activity against human recombinant TRPM8 expressed in CHO T-rex cells assessed as inhibition of WS12-induced calcium response pre-incubated for 20 mins before WS12 addition | B | 6.74 | pIC50 | 181 | nM | IC50 | ACS Med Chem Lett (2015) 6: 419-424 [PMID:25893043] |
| ChEMBL | Antagonist activity against human TRPM8 by single cell patch clamp electrophysiology | B | 6.99 | pIC50 | 103 | nM | IC50 | ACS Med Chem Lett (2015) 6: 419-424 [PMID:25893043] |
| ChEMBL | Voltage activation at room temperature | B | 6.99 | pIC50 | 103 | nM | IC50 | Data for DCP probe PF-05105679 |
| GtoPdb | - | - | 6.99 | pIC50 | 103 | nM | IC50 | ACS Med Chem Lett (2015) 6: 419-24 [PMID:25893043] |
| ChEMBL | Transients WS-12 activation | B | 7.53 | pIC50 | 29.6 | nM | IC50 | Data for DCP probe PF-05105679 |
| ChEMBL | Voltage activation at 12 °C | B | 7.86 | pIC50 | 13.8 | nM | IC50 | Data for DCP probe PF-05105679 |
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]
