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Assay Detail

CHEMBL674820

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Binding
Compound was tested by chromogenic assay for the inhibition of serine proteases like Porcine Elastase
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Chymotrypsin-like elastase family member 2A (CHEMBL2407)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.
Iijima K, Katada J, Yasuda E, Uno I, Hayashi Y.
J Med Chem (1999) 42 : 312 -323
PubMed 9925737 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.04 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108294 3 9.15
CHEMBL111705 1 6.70
CHEMBL320132 1 6.57
CHEMBL111745 1 5.57
CHEMBL110995 1 5.38
CHEMBL109601 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108294 IC50 = 0.7 nM 9.15
CHEMBL108294 IC50 = 8.6 nM 8.07
CHEMBL108294 IC50 = 14.0 nM 7.85
CHEMBL111705 IC50 = 200.0 nM 6.70
CHEMBL320132 IC50 = 270.0 nM 6.57
CHEMBL111745 IC50 = 2700.0 nM 5.57
CHEMBL110995 IC50 = 4200.0 nM 5.38
CHEMBL109601 IC50 = 710000.0 nM -