Compound name
WHI-P180
Protein family
Protein Kinase
Target name
RET
Affinity biochemical (nM)
4.5
Affinity on-target cellular (nM)
380
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001196a
SMILES
COC1=C(OC)C=C(C(NC2=CC=CC(O)=C2)=NC=N3)C3=C1
InChIKey
BNDYIYYKEIXHNK-UHFFFAOYSA-N
NCBI gene ID
5979
UniProt ID
P07949
Synonyms
PTC, CDHF12, RET51, CDHR16
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF assay (at Km = ATP)
Affinity Biochemical Source Knowledge
https://www.sciencedirect.com/science/article/pii/S0223523416300393?via%3Dihub
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
CellTiter-Glo assay (in BaF3 cells expressing KIF5B-RET)
Affinity on-target cellular source knowledge
https://www.sciencedirect.com/science/article/pii/S0223523416300393?via%3Dihub
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (DSF assay, SGC Frankfurt)
Selectivity platform number of targets
100
Selectivity remarks
Screened at 10 µM, closest target dTm(STK10) = 4.2K, all other targets dTm <4 K;
Selectivity Source Knowledge
https://www.pnas.org/doi/full/10.1073/pnas.0708800104#sec-3
Selectivity Number of Off-targets
1