Compound name
BI-1942
Protein family
Protease
Target name
CMA1@Protease
Affinity biochemical (nM)
0.4
CG-Set
Protease set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001112a
SMILES
CC[C@H](CC(O)=O)N1C(c2c(cccn2)N(Cc2cn(C)c3cc(C)cc(C)c23)C1=O)=O
InChIKey
PCJVXTDIDUMIRR-QGZVFWFLSA-N
NCBI gene ID
1215
UniProt ID
P23946
Synonyms
CYH, MCT1, chymase
Mode of action
Inhibitor
Negative control
No control available for probe
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay (inhibition of recombinant human chymase CMA1)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23659209/
Affinity biochemical relation
0
Selectivity platform
Protease panel (Eurofins)
Selectivity platform number of targets
35
Selectivity remarks
Screened at 10 µM, in-vitro potency of closest target: IC50(CTSG, cathepsin G) = 110 nM, >100-fold selective; Screened at 10 µM against 44 targets outside target family (Eurofins Safety Screen44TM), clean selectivity profile; Screened at 10 µM against 45 GPCRs (PDSP screen), in-vitro potencies of closest targets: Ki(HTR1D) = 1130.61 nM, Ki(OPRK1) = 4948.48 nM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI-1942
Selectivity Number of Off-targets
1