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 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]
