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Assay Detail

CHEMBL4380424

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant human chymase expressed in Pichia pastoris X-33 cells assessed as decrease in angiotensin 1 cleavage to angiotensin 2 incubated for 120 mins at 298 K by UPLC-MS analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Chymase (CHEMBL4068)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.
Li CY, Yap K, Swedberg JE, Craik DJ, de Veer SJ.
J Med Chem (2020) 63 : 816 -826
PubMed 31855419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.34 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4592765 1 8.00
CHEMBL4560112 1 7.48
CHEMBL4554739 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4592765 IC50 = 10.0 nM 8.00
CHEMBL4560112 IC50 = 33.0 nM 7.48
CHEMBL4554739 IC50 = 290.0 nM 6.54