Compound name
PF-06700841
Protein family
Protein Kinase
Target name
JAK1
Affinity biochemical (nM)
17
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001542aTs
SMILES
Cc1ccc(S(=O)(=O)O)cc1.Cn1cc(Nc2nccc(N3CC4CCC(C3)N4C(=O)[C@@H]3CC3(F)F)n2)cn1
InChIKey
FAKGOYNHHHOTEN-WTMFEIAXSA-N
NCBI gene ID
3716
UniProt ID
P23458
Synonyms
JAK1A, JTK3
Mode of action
inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Microfluidic assay (phosphorylation of synthetic peptide by recombinant human JAK1, at 1 mM ATP, Caliper Life Science)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00917
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Carna Biosciences)
Selectivity platform number of targets
306
Selectivity remarks
Screened at 1 µM, conc. ATP = Km, closest targets >90% of inhibition: AURKA/TPX2 (97%), TNK1 (94%), JAK3(92%), QIK(91%); Screened at 10 µM against a broad panel of receptors, ion channels, and transporters (CEREP Wide Ligand Profile screen), in-vitro potency of closest target: IC50(KDR) = 1600 nM, others <50% inhibition, IC50 follow-up in cell-based assay (NovaScreen): IC50(KDR) >30 µM (https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00917);
Selectivity Source Knowledge
https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.8b00917