Compound name
SPHINX31
Protein family
Protein Kinase
Target name
SRPK1
Affinity biochemical (nM)
17
Affinity on-target cellular (nM)
60
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000078b
SMILES
O=C(C1=CC=C(C2=CC=NC=C2)O1)NC(C=C(C(F)(F)F)C=C3)=C3N(CC4)CCN4CC5=CC=CC=N5
InChIKey
VURLRACCOCGFDB-UHFFFAOYSA-N
NCBI gene ID
6732
UniProt ID
Q96SB4
Synonyms
SFRSK1
Mode of action
Inhibitor
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)
Affinity on-target cellular source knowledge
https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.2c01705
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (DSF assay, SGC Frankfurt)
Selectivity platform number of targets
100
Selectivity remarks
Screened at 20 µM, closest targets: PHKG2 = 3.0 K, BRD4 = 7.6 K, MSSK1 = 5.2 K, clean; Differential scanning fluorimetry screen against 12 related kinases, at 12.5 µM: ΔTm(SRPK1) = 12.8°C; ΔTm(SRPK2, CLK1) = 6.7 °C, ΔTm(CLK4) = 5.7 °C; other splicing kinases <2°CScreened at 1 µM against 50 kinases, Radiolabeled ATP competition assay (MRC Dundee Kinase Centre), closest targets: SRPK1 (96% inhibition), highly selective;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acschembio.6b01048
Selectivity Number of Off-targets
2