Compound name
BMS 777607
Protein family
Protein Kinase
Target name
MST1R
Affinity biochemical (nM)
1.8
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000624a
SMILES
CCOC1=C(C(=O)N(C=C1)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F
InChIKey
VNBRGSXVFBYQNN-UHFFFAOYSA-N
NCBI gene ID
4486
UniProt ID
Q04912
Synonyms
CDw136, CD136
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzyme activity assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/jm801586s
Affinity biochemical relation
=
Selectivity platform
Ambit kinome screening platform
Selectivity platform number of targets
200
Selectivity remarks
Screened at 10 µM (Ambit phage-based competition binding assay), closest targets as % of contr.: FRK (0.55%), FLT4 (0.85%), FLT3 (0.05%), EPHA3 (0.1%), CSF1R (0.8%), BLK (0.35%), STK10 (0%), AURKB (0%), KIT (0%), LCK (0.2%), MUSK (0%), PDGFRA/B (0.2/0.7%), TEK (0.15%), NTRK1/2/3 (0.55/ 0.1/ 0.1%), KDR (0.2%), MKNK2 (0.75%); In vitro follow up of closest targets: IC50(MERTK) = 14 nM, IC50(FLT3) = 16 nM, IC50(AURKB) = 78 nM, IC50(LCK) = 120 nM, IC50(KDR) = 180 nM, IC50(NTRK1/2) = 290/ 190 nM, IC50(PKA) = 550, IC50 >2 µM for: BTK, CDK2E, EGFR, GSK3B, IGFR1R, IKK1/2, INSR, JAK2, MAPKAPK2, MAPK14, PIM1, PLK1/3
Selectivity Source Knowledge
https://doi.org/10.1021/jm801586s
Selectivity Number of Off-targets
20