Compound name
NVS-MALT1
Protein family
Protease
Target name
MALT1
Affinity biochemical (nM)
2.4
CG-Set
Other targets
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000239b
SMILES
CO[C@@H](C)c1c(Nc2ccc([C@H](N(C)C(=O)C3CCS(=O)(=O)CC3)C(F)(F)F)cc2)cnc2cc(Cl)nn12
InChIKey
NVGROBHDOYRPAN-FPTDNZKUSA-N
NCBI gene ID
10892
UniProt ID
Q9UDY8
Synonyms
MALT1, MLT
Mode of action
Allosteric inhibitor
Negative control
NVS-MALT1-C
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay (high salt)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/NVS-MALT1
Affinity biochemical relation
=
Selectivity platform
Protease assay, literature
Selectivity platform number of targets
16
Selectivity remarks
Screened at 10 µM, no cross reactivity among proteases owing to allosteric mechanism; Screened against 468 kinases(KinomeScan DiscoverX) at 1 µM, closest targets as % contr.: FLT3(N841I) (23%), CDK8 (39%), HIPK1 (40%), NEK3 (40%), MAST1 (43%), PIK3CA(E545K) (48%); Clean profile in screen against 45 GPCRs (PDSP screen) at 10 µM; Screened in kinase panel against 50 targets at 10 µM, closest targets: IC50(FLT3) = 3.5 µM; Screened against panel of 110 receptors, ion channels, enzymes and transporters, at 10 µM, closest target as % of inhibition: adenosine transporter AdT (52%);
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/NVS-MALT1
Selectivity Number of Off-targets
0