Compound name
NVP-BHG712
Protein family
Protein Kinase
Target name
EPHA2
Affinity biochemical (nM)
13
Affinity on-target cellular (nM)
3
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000143b
SMILES
Cc1ccc(C(=O)Nc2cccc(C(F)(F)F)c2)cc1Nc1nc(-c2cccnc2)nc2c1cnn2C
InChIKey
ZCCPLJOKGAACRT-UHFFFAOYSA-N
NCBI gene ID
1969
UniProt ID
P29317
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Microscale thermophoresis (MST) assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1002/cmdc.201800398
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
Kinobeads competition assays (Proteomics), literature
Selectivity platform number of targets
1483
Selectivity remarks
Closest targets: Kd(EPHA5) = 37.9 nM, other targets with low Kd values determined, however targets areof low- to no confidence; Cellular potency of closely related targets (NanoBRET assay in HEK293T cells): IC50(EPHA1) = 330 nM, IC50(EPHA3) = 1000 nM, IC50(EPHA4) = 100 nM, IC50(EPHA5) = 37 nM, IC50(EPHA6) = 2000 nM, IC50(EPHA7) = 2000 nM, IC50(EPHA8) = 12 nM, IC50(EPHB1) = 1000 nM, IC50(EPHB2) = 37 nM, IC50(EPHB3) = 330 nM, IC50(EPHB6) = 330 nM;Screened against 40 kinases in TR-FRET-based LanthaScreen™ and Caliper mobility shift assays, closest targets: IC50(RAF1) = 395 nM, IC50(c-Sarc) = 1266 nM, IC50(c-ABL) = 1667 nM, others >10 µM (PMID: 20803239)
Selectivity Source Knowledge
https://doi.org/10.1002/cmdc.201800398
Selectivity Number of Off-targets
1