Compound name
LOXO-195
Protein family
Protein Kinase
Target name
NTRK1
Affinity biochemical (nM)
3.7
Affinity on-target cellular (nM)
1.6
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000640a
SMILES
O=C(N[C@H](C)CCC1=NC=C(F)C=C1[C@]2([H])N3CCC2)C4=C5N(N=C4)C=CC3=N5
InChIKey
OEBIHOVSAMBXIB-SJKOYZFVSA-N
NCBI gene ID
4914
UniProt ID
P04629
Synonyms
TRK, TRKA, MTC
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
LanthaScreenTM Eu
Affinity Biochemical Source Knowledge
https://doi.org/10.1158/2159-8290.CD-17-0507
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Phospho-TRKA ELISA (inhibition of NTRK1 phosphorylation in NIH 3T3 cells)
Affinity on-target cellular relation
=
Selectivity platform
KinaseProfiler™ (Millipore)
Selectivity platform number of targets
228
Selectivity remarks
Screened at 1 µM, closest targets as % of contr.: BMX (15%), ROS1 (12%), TXK (14%), TNK2(10%)
Selectivity Source Knowledge
https://doi.org/10.1158/2159-8290.CD-17-0507
Selectivity Number of Off-targets
4