onvansertib [Ligand Id: 7918] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1738758 (Nms-1286937, NMS-1286937, NMS-P937, Onvansertib, PCM-075) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Inhibition of ALK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Inhibition of PKAalpha assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311, Q9UBU7] | ||||||||
| ChEMBL | Inhibition of CDC7/DBF4 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| ChEMBL | Inhibition of CDK1/CYCB assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] | ||||||||
| ChEMBL | Inhibition of CDK2/CYCA assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
| ChEMBL | Inhibition of CDK2/CYCE assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| ChEMBL | Inhibition of CDK4/CYCD1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Inhibition of CDK5/P25 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Inhibition of MPS1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Inhibition of EphA2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5] | ||||||||
| ChEMBL | Inhibition of PERK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of FGFR1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Inhibition of FAK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of GSK3-beta assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Inhibition of MET assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| High affinity immunoglobulin gamma Fc receptor I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5349] [UniProtKB: P12314] | ||||||||
| ChEMBL | Inhibition of IGFR1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
| ChEMBL | Inhibition of IKK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of IR assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Inhibition of MAPKAPK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Inhibition of ERK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of P38alpha assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Inhibition of MNK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Inhibition of MELK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 6.13 | pIC50 | 744 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683] | ||||||||
| ChEMBL | Inhibition of BUB1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Inhibition of TRKA assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Inhibition of PKCbeta assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] | ||||||||
| ChEMBL | Inhibition of ROS1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
| ChEMBL | Inhibition of PDK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition of AKT1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of Aur-A assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Inhibition of Aur-B assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of CHK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| eukaryotic elongation factor 2 kinase/Serine/threonine-protein kinase EEF2K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418] | ||||||||
| ChEMBL | Inhibition of EEF2K assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76] | ||||||||
| ChEMBL | Inhibition of Haspin assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] | ||||||||
| ChEMBL | Inhibition of MST4 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| NIMA related kinase 6/Serine/threonine-protein kinase NEK6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98] | ||||||||
| ChEMBL | Inhibition of NEK6 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84] | ||||||||
| ChEMBL | Inhibition of NIM1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
| ChEMBL | Inhibition of PAK4 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| 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 PIM1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Inhibition of PIM2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Biochemical Assay: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-gamma-ATP, and in the presence of their own optimal buffer and cofactors.At the end of the phosphorylation reaction, more than 98% cold ATP and radioactive ATP is captured by an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity.Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, then evaluated by beta-counting.Reagents/Assay Conditions i. Dowex Resin Preparation500 g of wet resin (SIGMA, custom prepared resin DOWEX 1x8 200-400 mesh, 2.5 Kg) are weighed out and diluted to 2 L in 150 mM sodium formate, pH 3.00.The resin is allowed to settle down. | B | 8.52 | pIC50 | 3 | nM | IC50 | US-8614220-B2. Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors (2013) |
| ChEMBL | Inhibition of PLK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862] |
| polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862] |
| ChEMBL | Inhibition of PLK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862] |
| ChEMBL | Inhibition of PLK3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| tousled like kinase 2/Serine/threonine-protein kinase tousled-like 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5404] [GtoPdb: 2243] [UniProtKB: Q86UE8] | ||||||||
| ChEMBL | Inhibition of TLK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Inhibition of KIT assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Inhibition of ACK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Inhibition of ABL assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Inhibition of BRK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Inhibition of JAK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of JAK3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| 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 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| 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 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | - | - | 6.29 | pIC50 | 510 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862] |
| ChEMBL | Inhibition of FLT3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 6.29 | pIC50 | 510 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Inhibition of RET assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Inhibition of Syk assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Inhibition of TYK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of ZAP70 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of VEGFR2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Inhibition of VEGFR3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862] |
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]
