Compound name
Linsitinib
Protein family
Protein Kinase
Target name
IGF1R
Affinity biochemical (nM)
35
Affinity on-target cellular (nM)
24
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000614a
SMILES
NC1=NC=CN2C1=C(C3=CC(N=C(C4=CC=CC=C4)C=C5)=C5C=C3)N=C2[C@H]6C[C@@](C)(O)C6
InChIKey
PKCDDUHJAFVJJB-VLZXCDOPSA-N
NCBI gene ID
3480
UniProt ID
P08069
Synonyms
JTK13, CD221, IGFIR, MGC18216, IGFR
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay (100 µM ATP)
Affinity Biochemical Source Knowledge
https://doi.org/10.4155/fmc.09.89
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblot (IGF-1-dependent autophosphorylation of IGF-1R in LISN cells)
Affinity on-target cellular relation
=
Selectivity platform
Kinobeads, literature
Selectivity platform number of targets
224
Selectivity remarks
Screened at 1 µM, closest targets as % inhibition: MAP4K2 (99%), MET(86%); Screened also with ProfilerPro® Kinase Selectivity Assay Kit (Caliper Life Sciences) at 1 µM, 88 kinases <50% inhibition, clean in IC50 follow up assay: IC50 >10 µM (PMID: 21425998)
Selectivity Source Knowledge
https://doi.org/10.1126/science.aan4368
Selectivity Number of Off-targets
2