Compound name
MK-8033
Protein family
Protein Kinase
Target name
MST1R
Affinity biochemical (nM)
7
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001851a
SMILES
Cn1cc(-c2cnc3ccc4ccc(CS(=O)(=O)NCc5ccccn5)cc4c(=O)c3c2)cn1
InChIKey
VMJFTOSOFDEKTM-UHFFFAOYSA-N
NCBI gene ID
4486
UniProt ID
Q04912
Synonyms
CDw136, CD136
Mode of action
inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23379595/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Millipore)
Selectivity platform number of targets
221
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: MET(95%), RON(93%), MER (67%), FLT4(63%), FGFR3(62%), FES(60%), full screening data available in supplemental information, Table S2; In-vitro follow up of closest targets (TR-FRET assay): IC50(MER) = 880 nM, IC50(FLT4) = 920 nM, IC50(FGFR3) = 1000 nM, IC50(FGFR3) = 1700 nM, IC50(KDR) = 1700 nM, IC50(FES) >10000 nM, https://pubmed.ncbi.nlm.nih.gov/23379595/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23379595/
Selectivity Number of Off-targets
3