Compound name
LDC1267
Protein family
Protein Kinase
Target name
AXL
Affinity biochemical (nM)
29
Affinity on-target cellular (nM)
19
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000147b
SMILES
CCOc1cn(-c2ccc(F)cc2C)nc1C(=O)Nc1ccc(Oc2ccnc3cc(OC)c(OC)cc23)c(F)c1
InChIKey
ISPBCAXOSOLFME-UHFFFAOYSA-N
NCBI gene ID
558
UniProt ID
P30530
Synonyms
UFO, JTK11, Tyro7, ARK
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF assay
Affinity Biochemical Source Knowledge
https://doi.org/0.1038/nature12998
Affinity biochemical relation
=
Affinity on-target cellular definition
Kd
Affinity on-target cellular assay type
Quantitative chemical proteomics in Hs578t cells
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
465
Selectivity remarks
Screened at 1 µM, closest targets with <10% of contr.: ABL1, BLK, DDR1, FLT3, KIT, LCK, STK10, MAP2K5, MET, HIPK4, AURKB/C, FER, HCK, MST1R, CDK19, FRK, SRC, TIE1, CHEK2, MUSK, CDK8, CSF1R, EPHB6, PDGFRB, ROS1, NRTK1/3, MAP4K5, and mutants; Cellular selectivity (quantitative chemical proteomics, cell-based phosphorylation and proliferation assays in Hs578t cells), closest targets: Kd(cMET) = 13 nM,Kd(FER) = 107 nM, Kd(MAP2K5) = 124 nM, Kd(ABL1) = 154 nM, Kd(SRC) = 217 nM;
Selectivity Source Knowledge
https://doi.org/0.1038/nature12998
Selectivity Number of Off-targets
29