timcodar [Ligand Id: 10868] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2059028 (Timcodar, Vx-853, VX-853) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 mins using [3H]-estrone sulfate as substrate by rapid filtration technique | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| FKBP prolyl isomerase 1A/Peptidyl-prolyl cis-trans isomerase FKBP1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1902] [GtoPdb: 2609] [UniProtKB: P62942] | ||||||||
| ChEMBL | Binding affinity to FKBP12 by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 4114-4122 [PMID:22455444] |
| FKBP prolyl isomerase 4/Peptidyl-prolyl cis-trans isomerase FKBP4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4050] [GtoPdb: 3176] [UniProtKB: Q02790] | ||||||||
| ChEMBL | Binding affinity to FKBP52 FK1 domain by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 4114-4122 [PMID:22455444] |
| FKBP prolyl isomerase 5/Peptidyl-prolyl cis-trans isomerase FKBP5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2052031] [GtoPdb: 3175] [UniProtKB: Q13451] | ||||||||
| ChEMBL | Binding affinity to FKBP51 FK1 domain by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 4114-4122 [PMID:22455444] |
ChEMBL data shown on this page come from version 36:
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]
