EUB0001632a_CDK12

Screened at 10 µM, closest targets as % of inhibition (using ATP = Km app): GSK3B (89%), GSK3A (82.2%), CSNK1E(48.9%); Screened at 10 µM against 31 kinases (Adapta Assay using ATP = Km app), closest targets as % of inhibition: LRRK2(I2020T, 100%), LRRK2 (100%), LRRK2(R1441C, 96.1%), LRRK2 (G2019S, 95%), SPHK2(67.7%), PIK3CD/PIK3R1 (p110 delta/p85 alpha, 66%), PIK3C2B (PI3K-C2 beta, 64.1%), CDK9/cyclin T1 (63.9%), SPHK1 (53.7%), GSG2 (45%), https://pubmed.ncbi.nlm.nih.gov/31668947/; In-vitro potency (enzymatic assay on full-lenght LRRK2): IC50(LRRK2) >10 µM, https://pubmed.ncbi.nlm.nih.gov/31668947/; Screened at 10 µM against 162 kinases (LanthaScreen Eu Kinase Binding Assay), closest targets as % of inhibition: TAOK1 (31.8%), CDK8/cyclinC (17%), CDK16(PCTK1)/cyclinY (15%), NLK(13.4%), CLK4(12.3%), SIK3(12.2%), https://pubmed.ncbi.nlm.nih.gov/31668947/; Screened at 10 µM against 20 kinases (Rxn Biology kinase assay using 10 µM ATP), targets as % of inhibition: GSK3B (96.5%), GSK3A (90.6%), CDK6/cyclin D1 (83.4%), CDK6/cyclin D3 (52.7%), CDK4/cyclin D1(46.7%), CDK4/cyclin D3(46.3%), MEK2(8.7%), AKT3(6.7%), MAPK1(5.8%), MEK1(4.5%), AXL(4.1%), EGFR(3.4%), ERBB2(2.6%), AKT2(1.6%), AKT1(0.2%), ERK1(-5.8%), MAPK15 (-25.6%), MAPK7(-29.8%), MET(-31.5%), MAPK7(-42.4%), https://pubmed.ncbi.nlm.nih.gov/31668947/;