GSK2798745 [Ligand Id: 12557] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4470585 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0] | ||||||||
| ChEMBL | Antagonist activity at human TRPV4 | B | 8.7 | pIC50 | 2 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1498-1502 [PMID:34531959] |
| ChEMBL | Inhibition of human TRPV4 expressed in baculovirus infected HEK/MSR 2 cells pre-incubated for 10 mins followed by GSK634775A addition by Fura-2 dye based FLIPR assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1228-1233 [PMID:31413810] |
| ChEMBL | Antagonist activity at human TRPV4 | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2019) 62: 9270-9280 [PMID:31532662] |
| GtoPdb | - | - | 8.82 | pIC50 | 1.5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1228-1233 [PMID:31413810] |
| TRPV4/Transient receptor potential cation channel subfamily V member 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2775] [GtoPdb: 510] [UniProtKB: Q9ERZ8] | ||||||||
| ChEMBL | Inhibition of rat TRPV4 expressed in baculovirus infected HEK/MSR 2 cells pre-incubated for 10 mins followed by GSK634775A addition by Fura-2 dye based FLIPR assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1228-1233 [PMID:31413810] |
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]
