PF-4840154 [Ligand Id: 6309] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1818218 (PF-4840154) |
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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 human ERG expressed in human HEK293 cells by patch-clamp electrophysiology | B | 6.24 | pIC50 | 580 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4857-4859 [PMID:21741838] |
| TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] | ||||||||
| GtoPdb | Calcium imaging | - | 7.6 | pEC50 | 25.1 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 4857-9 [PMID:21741838] |
| ChEMBL | Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as calcium influx measured at every 1 second for 60 seconds by fluorescence analysis | F | 7.64 | pEC50 | 23 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 4857-4859 [PMID:21741838] |
| TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | J Gen Physiol (2018) 150: 751-762 [PMID:29703838] |
| ChEMBL | Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as calcium influx measured at every 1 second for 60 seconds by fluorescence analysis | F | 7.01 | pEC50 | 97 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 4857-4859 [PMID:21741838] |
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]
