Compound name
MSC2711186A
Protein family
Protein Kinase
Target name
SRPK1
Affinity biochemical (nM)
2.7
Affinity on-target cellular (nM)
44
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001048a
SMILES
Fc2c1nc([nH]c1ccc2Cl)-c3nc(ccn3)NCc4c(nccc4)N(S(=O)(=O)C)C
InChIKey
WBFJDKLBAAHKIL-UHFFFAOYSA-N
NCBI gene ID
6732
UniProt ID
Q96SB4
Synonyms
SFRSK1
Mode of action
Inhibitor
Negative control
MSC2705360A
Affinity biochemical definition
IC50
Affinity biochemical assay type
Biochemical activity assay (Reaction Biology)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.2c01705
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (in HEK293T cells, lysed mode)
Affinity on-target cellular source knowledge
https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.2c01705
Affinity on-target cellular relation
=
Selectivity platform
Kinome Scan (Reaction Biology)
Selectivity platform number of targets
395
Selectivity remarks
Screened at 1 µM, closest targets as % of control: STK2 (3.83%), SRPK1 (8.76%), SRPK2 (13.94%), PIM1 (54.68%), PKCe(55.07%), PKN1(55.56%); In-vitro potency of closest targets (Radioactive assay, Reaction Biology): IC50(CLK1) >10 µM, IC50(CLK2) >10 µM, IC50(CLK3) >10 µM, IC50(CLK4) >10 µM, IC50(DYRK1A) >10 µM, IC50(DYRK1B) >10 µM, IC50(DYRK2) >10 µM, IC50(DYRK3) >10 µM, https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.2c01705#;
Selectivity Source Knowledge
https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.2c01705