prexasertib [Ligand Id: 9549] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL3544911 (LY2606368, Prexasertib) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| 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] |
| 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] | ||||||||
| 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] |
| 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 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]
