Compound name
Takinib
Protein family
Protein Kinase
Target name
MAP3K7
Affinity biochemical (nM)
5.46
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002327a
SMILES
CCCn1c(NC(=O)c2cccc(C(N)=O)c2)nc2ccccc21
InChIKey
UOZVVPXKJGOFIG-UHFFFAOYSA-N
NCBI gene ID
6885
UniProt ID
O43318
Synonyms
MEKK7
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric assay (Activity of purified TAK1-TAB1 protein using 5 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28820959/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (MRC Dundee)
Selectivity platform number of targets
140
Selectivity remarks
Screened at 10 µM, closest targets as % on control: MAP3K7 (2%), CLK2 (4%), IRAK1 (4%), IRAK4 (7%), GCK (9%), MINK1 (9%), CSNK1G2 (13%), full screening data available as supporting information; In-vitro potency (enzymatic assay, MRC Dundee): IC50(MAP3K7) = 9.5 nM, IC50(IRAK4) = 120 nM, IC50(IRAK1) = 390 nM, IC50(GCK) = 430 nM, IC50(CLK2) = 430 nM, IC50(MINK1) = 1900 nM, https://pubmed.ncbi.nlm.nih.gov/28820959/; Kinase proteome profiling in RA-FLS cells, against 45 kinases, closest targets as % of activity: LCK (42.6%), full screening data available as supporting info, https://pubmed.ncbi.nlm.nih.gov/31847895/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28820959/
Selectivity Number of Off-targets
5