Compound name
(5Z)-7-Oxozeaenol
Protein family
Protein Kinase
Target name
KDR
Affinity biochemical (nM)
52
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002167a
SMILES
COc1cc(O)c2c(c1)/C=C\C[C@H](O)[C@H](O)C(=O)/C=C\C[C@H](C)OC2=O
InChIKey
NEQZWEXWOFPKOT-UXGSFGIESA-N
NCBI gene ID
3791
UniProt ID
P35968
Synonyms
FLK1, VEGFR, VEGFR2, CD309
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/17676571/
Affinity biochemical relation
=
Selectivity platform
KINOMEscan (DiscoverX)
Selectivity platform number of targets
456
Selectivity remarks
Screened at 1 µM and 10 µM against 456 kinases (KinomeScan DiscoverX), closest targets as % of inhibition at 1 µM: RIOK3 (74%), MAP2K1 (0.65%), MAP2K2 (0.75%), PDGFRB (1.5%), MAP2K5 (0.2%), FLT4(8.2%), MAP2K4 (19%), FLT1(16%), FLT3(4.2%), KIT (20%), TGFBR2(3.8%), STK36 (7.1%), MAP2K3 (22%), ACVR1 (21%), MAP3K20 (5.6%), PRKD2 (72%), RSK4 (34%), MAP3K7 (58%), BIKE (68%), KDR (78%), CDKL2 (76%), screening data for 10 µM available as supporting information;
Screened at 1 µM, closest targets as % of control: MAP2K5 (0.2%), MAP2K1 (0.7%), MAP2K2 (0.8%), KIT (D816V, 1%), GAK (10%), FLT3(N841I), TGFBR2 (3.8%), FLT3 (4.2%), FLT3 (ITD, 4.2%), MLTK (5.6%), STK36 (7.1%), FLT3(D835Y, 8.0%), FLT4 (8.2%), FLT3 (K663Q, 8.6%), full screening data available, also screened at 10 µM, 22 kinases with <10% of control https://lincs.hms.harvard.edu/db/datasets/20211/results;
Screened in KiNative profiling against 170 kinases, using SK-CO-1 cells, closest targets as % of inhibition: ARAF (85.5%), MAP4K1 (77.3%), MAP2K1 (89.4%), MAP2K2 (95%), MAP2K5 (86.8%), TAK1 (90%), MAP3K20 (87.5%), https://www.sciencedirect.com/science/article/pii/S0968089616312378?via%3Dihub;
Screened at 1 µM, closest targets as % of control: MAP2K5 (0.2%), MAP2K1 (0.7%), MAP2K2 (0.8%), KIT (D816V, 1%), GAK (10%), FLT3(N841I), TGFBR2 (3.8%), FLT3 (4.2%), FLT3 (ITD, 4.2%), MLTK (5.6%), STK36 (7.1%), FLT3(D835Y, 8.0%), FLT4 (8.2%), FLT3 (K663Q, 8.6%), full screening data available, also screened at 10 µM, 22 kinases with <10% of control https://lincs.hms.harvard.edu/db/datasets/20211/results;
Screened in KiNative profiling against 170 kinases, using SK-CO-1 cells, closest targets as % of inhibition: ARAF (85.5%), MAP4K1 (77.3%), MAP2K1 (89.4%), MAP2K2 (95%), MAP2K5 (86.8%), TAK1 (90%), MAP3K20 (87.5%), https://www.sciencedirect.com/science/article/pii/S0968089616312378?via%3Dihub;
Selectivity Source Knowledge
https://www.sciencedirect.com/science/article/pii/S0968089616312378?via%3Dihub
Selectivity Number of Off-targets
9