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Assay Detail

CHEMBL815149

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

Binding
Compound was evaluated for inhibition of amidolytic activity for chromogenic substrate trypsin
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypsin II (CHEMBL4472)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1.
Levy OE, Semple JE, Lim ML, Reiner J, Rote WE, Dempsey E, Richard BM, Zhang E, Tulinsky A, Ripka WC, Nutt RF.
J Med Chem (1996) 39 : 4527 -4530
PubMed 8917638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.88 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL141676 1 8.92
CHEMBL342838 2 7.16
CHEMBL344204 1 6.48
CHEMBL138441 1 5.81
CHEMBL342914 2 4.82
CHEMBL342604 1 4.22
CHEMBL141424 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL141676 IC50 = 1.2 nM 8.92
CHEMBL342838 IC50 = 69.7 nM 7.16
CHEMBL342838 IC50 = 113.0 nM 6.95
CHEMBL344204 IC50 = 329.0 nM 6.48
CHEMBL138441 IC50 = 1550.0 nM 5.81
CHEMBL342914 IC50 = 15100.0 nM 4.82
CHEMBL342914 IC50 = 45800.0 nM 4.34
CHEMBL342604 IC50 = 60700.0 nM 4.22
CHEMBL141424 IC50 = 64800.0 nM 4.19