Compound name
(5Z)-7-Oxozeaenol
Protein family
Protein Kinase
Target name
MAP3K7
Affinity biochemical (nM)
8.1
Affinity on-target cellular (nM)
100
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
6885
UniProt ID
O43318
Synonyms
MEKK7
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/12624112/
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Immunoblot assay (using catalytically active FLAG-tagged TAK1 together with TAB1 in HEK293 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/12624112/
Affinity on-target cellular 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