Compound name
BIX02188
Protein family
Protein Kinase
Target name
MAP2K5
Affinity biochemical (nM)
4.3
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001899a
SMILES
CN(Cc1cccc(c1)NC(=C1C(=O)Nc2c1ccc(c2)C(=O)N)c1ccccc1)C
InChIKey
FSZPIAXLCCQFCM-UHFFFAOYSA-N
NCBI gene ID
5607
UniProt ID
Q13163
Synonyms
MEK5, MAPKK5, HsT17454
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/18834865/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (University of Dundee and Invitrogen Corporation)
Selectivity platform number of targets
79
Selectivity remarks
Screened at 3 µM (Dundee panel) and 10 µM (Invitrogen panel), closest targets as % of control: CSF1R (3%, at 10 µM), SRC (3%, at 3 µM), LCK (8%, at 10 µM), other >10% of control, full screening data available in paper; In-vitro potency (enzymtic assay): IC50(ABL1) = 2100 nM, IC50(CSF1R) = 280 nM, IC50(FGFR1) > 10000 nM, IC50(JAK3) = 7800 nM, IC50(KIT) = 550 nM, IC50(LCK) = 390 nM, IC50(MAPK14) = 3900 nM, IC50(RPS6KA3) = 4100 nM, IC50(RPS6KA6) = 3200 nM, IC50(SRC) = 8900 nM, https://pubmed.ncbi.nlm.nih.gov/18834865/;
Screened at 20 µM, against 100 kinases, DSF panel (in-house), closest targets: dTm(ABL1) =3.1 K, dTm(FGFR3) = 4.6 K, dTm(FLT1) = 3.1 K, dTm(GSK3B) = 4.9K, dTm(MELK) = 7.6 K, dTm(STK10) = 6.1 K, dTm(BMP2K) = 4.9 K, in-house data
Screened at 20 µM, against 100 kinases, DSF panel (in-house), closest targets: dTm(ABL1) =3.1 K, dTm(FGFR3) = 4.6 K, dTm(FLT1) = 3.1 K, dTm(GSK3B) = 4.9K, dTm(MELK) = 7.6 K, dTm(STK10) = 6.1 K, dTm(BMP2K) = 4.9 K, in-house data
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/18834865/
Selectivity Number of Off-targets
3