prexasertib [Ligand Id: 9549] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3544911 (Ly-2606368, LY-2606368, LY2606368, Prexasertib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111345] [GtoPdb: 1545, 1541, 1543] [UniProtKB: P54619, Q13131, Q9Y478] | ||||||||
| ChEMBL | Inhibition of AMPKalpha1beta1gamma1 (unknown origin) using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 6.99 | pIC50 | 101.62 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDK1 (unknown origin) using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of CDK2 (unknown origin) using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] | ||||||||
| ChEMBL | Inhibition of NUAK1 (unknown origin) | B | 7.19 | pIC50 | 64 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Inhibition of p70S6K (unknown origin) using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 6.42 | pIC50 | 382.18 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of CHK1 (unknown origin) | B | 9 | pIC50 | <1 | nM | IC50 | Eur J Med Chem (2021) 215: 113268-113268 [PMID:33636537] |
| ChEMBL | Inhibition of CHK1 (unknown origin) | B | 9 | pIC50 | <1 | nM | IC50 | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| GtoPdb | Biochemical assay using purified enzyme. | - | 9.05 | pIC50 | 0.9 | nM | IC50 | Mol Cancer Ther (2015) 14: 2004-13 [PMID:26141948] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged CHK1 (M1 to T476 residues) expressed in baculovirus infected insect cells using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 9.25 | pIC50 | 0.56 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017] | ||||||||
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged CHK2 (M1 to L543 residues) expressed in baculovirus infected insect cells using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 7.49 | pIC50 | 32.57 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| ChEMBL | Inhibition of CHK2 (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2022) 230: 114109-114109 [PMID:35051747] |
| GtoPdb | Enzyme assay | - | 8.1 | pIC50 | 8 | nM | IC50 | Mol Cancer Ther (2015) 14: 2004-13 [PMID:26141948] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Inhibition of recombinant human full length N-terminal His-tagged PIM1 (1 to 313 residues) expressed in baculovirus expression system using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Inhibition of PIM3 (unknown origin) incubated for 60 mins using biotin-labelled STK substrate-1 as substrate by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Inhibition of BLK (unknown origin) using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 5.36 | pIC50 | 4409 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Inhibition of LCK (unknown origin) incubated for 60 mins by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Inhibition of LYN (unknown origin) incubated for 60 mins by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged FLT3 (M1 to N541 residues) expressed in HEK293 cells using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay | B | 6.41 | pIC50 | 385.98 | nM | IC50 | Eur J Med Chem (2019) 173: 44-62 [PMID:30986571] |
| ribosomal protein S6 kinase A1 in Human [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| GtoPdb | Enzyme assay | - | 8.05 | pIC50 | 9 | nM | IC50 | Mol Cancer Ther (2015) 14: 2004-13 [PMID:26141948] |
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]
