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 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]
