Compound name
GNF2
Protein family
Protein Kinase
Target name
ABL1
Affinity biochemical (nM)
9
Affinity on-target cellular (nM)
182
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000875a
SMILES
NC(C1=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=CC=C1)=O
InChIKey
WEVYNIUIFUYDGI-UHFFFAOYSA-N
NCBI gene ID
25
UniProt ID
P00519
Synonyms
JTK7, c-ABL, p150
Mode of action
Allosteric Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay (SH3SH2SH1 domain, Abl64-515)
Affinity Biochemical Source Knowledge
https://www.sciencedirect.com/science/article/pii/S1570963909003677?via%3Dihub
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
ELISA (autophosphorylation of Bcr-Abl-p210, wt, BAF3 cells)
Affinity on-target cellular source knowledge
https://www.sciencedirect.com/science/article/pii/S1570963909003677?via%3Dihub
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Millipore)
Selectivity platform number of targets
234
Selectivity remarks
Screened at 1 µM, closest targets as % of residual activity: RPS6KA3 (57%), CSF1R (74%), STK24 (74%), MELK (74%), compound also screened at 10 µM, https://pubmed.ncbi.nlm.nih.gov/23398362/, full-screening data available at Chembl;
Screened at 10 µM, against 63 kinases, radioenzymatic kinase assays (Upstate KinaseProfiler™), clean selectivity profile, https://www.nature.com/articles/nchembio760;
Screened at 10 µM, against 63 kinases, radioenzymatic kinase assays (Upstate KinaseProfiler™), clean selectivity profile, https://www.nature.com/articles/nchembio760;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23398362/
Selectivity Number of Off-targets
0