fimsosertib [Ligand Id: 14355] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5174716 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918] | ||||||||
| ChEMBL | Inhibition of HPK1 in human Jurkat E6.1 cells assessed as inhibition of SLP76 phosphorylation treated for 4 hrs by HTRF assay | B | 6 | pIC50 | <1000 | nM | IC50 | J Med Chem (2022) 65: 8065-8090 [PMID:35696642] |
| ChEMBL | Inhibition of HPK1 (unknown origin) preincubated for 15 mins measured after 90 mins by ADP-Glo kinase assay | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (2022) 65: 8065-8090 [PMID:35696642] |
| ChEMBL | Inhibition of HPK1 in human Jurkat E6.1 cells assessed as phosphorylation of SLP76 at serine 376 residue incubated for 4 hrs by HTRF assay | B | 7 | pIC50 | <100 | nM | IC50 | Eur J Med Chem (2023) 248: 115064-115064 [PMID:36621137] |
| GtoPdb | - | - | 8 | pIC50 | <10 | nM | IC50 | Eur J Med Chem (2023) 248: 115064 [PMID:36621137] |
| ChEMBL | Inhibition of HPK1 (unknown origin) incubated for 15 mins by ADP-Glo kinase assay | B | 8 | pIC50 | <10 | nM | IC50 | Eur J Med Chem (2023) 248: 115064-115064 [PMID:36621137] |
| ChEMBL | Inhibition of HPK1 (unknown origin) | B | 8 | pIC50 | <10 | nM | IC50 | J Med Chem (2023) 66: 16201-16221 [PMID:37990878] |
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]
