Compound name
OTS964
Protein family
Protein Kinase
Target name
PBK
Affinity biochemical (nM)
28
Affinity on-target cellular (nM)
100
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000055a
SMILES
Cc1cc(O)c(-c2ccc([C@@H](C)CN(C)C)cc2)c2c1[nH]c(=O)c1sccc12
InChIKey
XCFRUAOZMVFDPQ-AWEZNQCLSA-N
NCBI gene ID
55872
UniProt ID
Q96KB5
Synonyms
TOPK, FLJ14385, Nori-3, SPK, CT84
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzyme activity assay
Affinity Biochemical Source Knowledge
https://www.science.org/doi/10.1126/scitranslmed.3010277?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Western Blot (autophosphorylation of TOPK at Thr9 in T47D cells)
Affinity on-target cellular source knowledge
https://www.science.org/doi/10.1126/scitranslmed.3010277?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed
Affinity on-target cellular relation
<
Selectivity platform
Kinase panel (Eurofins)
Selectivity platform number of targets
412
Selectivity remarks
Screened at 1 µM, closest targets as % of control: TYK2 (20%), EGFR(L861Q, 24%), EGFR(L858R, 27%), full screening data available as supplement information;
Screened at 2 µM against 60 kinases, HotSpot assay platform (Reaction Biology), closest targets as % inhibition: SRC (87.6%), FLT3 (72.1%), LYN (77.4%), https://www.science.org/doi/10.1126/scitranslmed.3010277?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed;
Screened at 2 µM against 60 kinases, HotSpot assay platform (Reaction Biology), closest targets as % inhibition: SRC (87.6%), FLT3 (72.1%), LYN (77.4%), https://www.science.org/doi/10.1126/scitranslmed.3010277?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%20%200pubmed;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/36104565/
Selectivity Number of Off-targets
0