Compound name
BIX02189
Protein family
Protein Kinase
Target name
MAPK7
Affinity biochemical (nM)
59
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001900a
SMILES
CN(C)CC1=CC(=CC=C1)NC(=C2C3=C(C=C(C=C3)C(=O)N(C)C)NC2=O)C4=CC=CC=C4
InChIKey
HOMJAAIVTDVQJA-UHFFFAOYSA-N
NCBI gene ID
5598
UniProt ID
Q13164
Synonyms
BMK1, ERK5
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 (4%, at 10 µM), SRC (6%, at 3 µM), LCK (6%, at 10 µM), RPS6KA6 (6%, at 10 µM) other >10% of control, full screening data available in paper; In-vitro potency (enzymatic assay): IC50(ABL1) = 2400 nM, IC50(CSF1R) = 46 nM, IC50(FGFR1) = 1000 nM, IC50(JAK3) = 440 nM, IC50(KIT) = 1100 nM, IC50(LCK) = 250 nM, IC50(MAPK14) = 3700 nM, IC50(RPS6KA3) = 2100 nM, IC50(RPS6KA6) = 990 nM, IC50(SRC) = 7600 nM, https://pubmed.ncbi.nlm.nih.gov/18834865/;
Screened at 20 µM, against 100 kinases, DSF panel (in-house), closest targets: dTm(ABL1) = 3.2 K, dTm(FGFR3) = 4.5 K, dTm(MAP2K4) = 3.2 K, dTm(MAPK14) = 3.1K, dTm(FLT1) = 3.2 K, dTm(RPSKKA1) = 3.2 K, dTm(STK10) = 3.5 K, in-house data
Screened at 20 µM, against 100 kinases, DSF panel (in-house), closest targets: dTm(ABL1) = 3.2 K, dTm(FGFR3) = 4.5 K, dTm(MAP2K4) = 3.2 K, dTm(MAPK14) = 3.1K, dTm(FLT1) = 3.2 K, dTm(RPSKKA1) = 3.2 K, dTm(STK10) = 3.5 K, in-house data
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/18834865/
Selectivity Number of Off-targets
4