BI-1942

BI-1942 : Inhibitor of CMA1

Structure

Information

  • CMA1
  • Inhibitor
  • 100 nM

In Vitro Validations

Uniprot ID: P23946
Target Class: Enzyme
Target SubClass: Peptidase
Potency: IC50
Potency Value: 0.4 nM
Potency Assay: Inhibition of recombinant human CMA1
PDB ID for probe-target interaction (3D structure): 3S0N
Target aliases:
Chymase, CYM, CYH, CMA1, CMA1_HUMAN, Mast cell pro ...

DOI Reference: 10.1021/jm400138z

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
Selectivity within target family: Eurofins protease panel (35 at 10 µM): Only off-target is CTSG (cathepsin G, IC50 = 110 nM, > 100-fold selective). Selectivity outside target family: Eurofins SafetyScreen (44) at 10 µM: clean.
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SERP ratings and comments


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