Compound name
BMS 986165
Protein family
Protein Kinase
Target name
TYK2
Affinity biochemical (nM)
0.2
Affinity on-target cellular (nM)
2
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001543a
SMILES
[2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncn(C)n2)c1OC
InChIKey
BZZKEPGENYLQSC-FIBGUPNXSA-N
NCBI gene ID
7297
UniProt ID
P29597
Synonyms
JTK1
Mode of action
Allosteric inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF assay (TYK2, JH2 domain with 1 mM ATP)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00444
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
STAT-dependent luciferase reporter assay in PBMCs (IFNα-stimulation, measuring STAT5 phosphorylation in CD3+ T-cells as end point, TYK2/JAK1 dependent signaling)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/31318208/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (literature)
Selectivity platform number of targets
249
Selectivity remarks
All >1000-fold selective except BMPR2 (IC50 = 193 nM, ~960-fold selective); Selective within JAK family (HTRF assay, 1 mM ATP): IC50(JAK1) >10 µM, IC50(JAK2) >10 µM, IC50(JAK3) >10 µM, IC50(TYK2, JH1 domain) >10 µM, IC50(TYK2, JH2 domain) = 0.2 nM (https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00444);
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00444