Compound name
SGC-GAK-1
Protein family
Protein Kinase
Target name
GAK
Affinity biochemical (nM)
1.9
Affinity on-target cellular (nM)
120
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000207b
SMILES
COc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
InChIKey
AUOSKLDNVNGKRR-UHFFFAOYSA-N
NCBI gene ID
2580
UniProt ID
O14976
Synonyms
DNAJC26
Mode of action
Inhibitor
Negative control
SGC-GAK-1N
Affinity biochemical definition
Kd
Affinity biochemical assay type
Competition binding assay (DiscoverX)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.8b01213
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 1 µM, in vitro follow-up of closest targets: Kd(RIPK2) = 110 nM, Kd(ADCK3) = 190 nM, Kd(NLK) = 520 nM, Kd(ACVR1) = 980 nM; Cellular selectivity: IC50(RIPK2) = 360 nM (NanoBRET assay), others not tested;
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.8b01213
Selectivity Number of Off-targets
4