Compound name
XMU-MP-1
Protein family
Protein Kinase
Target name
STK3
Affinity biochemical (nM)
11
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000178b
SMILES
CN1C(=O)c2sccc2N(C)c2nc(Nc3ccc(S(N)(=O)=O)cc3)ncc21
InChIKey
YRDHKIFCGOZTGD-UHFFFAOYSA-N
NCBI gene ID
6788
UniProt ID
Q13188
Synonyms
MST2, KRS1
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
Competition binding assay (DiscoverX)
Affinity Biochemical Source Knowledge
https://doi.org/10.1126/scitranslmed.aaf2304
Affinity biochemical relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 1 µM, S(10) = 0.05, closest targets as % of contr.: ABL (M351T phosph.) (5.5%), ABL (Q252H phosph.) (6.8%), ABL (T315I phosph.) (1.6%), AURKA (0.05%), AURKB (3.4%), DCAMKL1 (8.3%), MAP3K2 (2.6%), MAP3K3 (2%), JAK1 (JH2 pseudokinase domain) (4.3%), STK24 (0.9%), STK26 (0.6%), PIK3CG (0.15%), PIP5K1C (10%), PIP5K2C (8%), RIPK4 (9.5%), TAOK1 (2.6%), TAOK2 (3.4%), TAOK3 (4.5%), TYK2 (JH1 catalytic domain, 2.7%), ULK2 (4.8%); Follow-up Kds and IC50s: Kd/IC50(ABL, M351T phosph.) = 42/ 17.6 nM, KD/IC50(ABL (Q252H phosph.) = 24/ 11.6 nM, Kd/IC50(ABL, T315I phosph.) = 14/ 16.6 nM, Kd/IC50 (AURKA) = 13/ 19.4 nM, Kd/IC50(AURKB) = 40/ 19.4 nM, Kd/IC50(DCAMKL1) = 25/ 27.9 nM, Kd/IC50(MAP3K2) = 19/ 79.6 nM, Kd/IC50(MAP3K3) = 27/ 38.4 nM, Kd/IC50(JAK1, JH2 pseudokinase domain) = 22/ 38.7 nM, Kd/IC50(STK24) = 18/ 44.8 nM, Kd/IC50(STK26) = 16/ 27.3 nM, Kd/IC50(PIK3CG) = 4.8/ 38.4 nM, Kd/IC50(PIP5K1C) = 77/ 436 nM, Kd(PIP5K2C) = 34 nM, Kd(RIPK4) = 140 nM, Kd/IC50(TAOK1) = 180/ 165 nM, Kd/IC50(TAOK2) = 100/ 134 nM, Kd/IC50(TAOK3) = 610/ 254 nM, Kd/IC50(TYK2, JH1 catalytic domain) = 610/ 254 nM, Kd/IC50(ULK2) = 35/ 41.5 nM;
Selectivity Source Knowledge
https://doi.org/10.1126/scitranslmed.aaf2304
Selectivity Number of Off-targets
20