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Assay Detail

CHEMBL865715

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

Binding
Inhibition of trypsin
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Trypsin (CHEMBL2095204)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.
Mack H, Baucke D, Hornberger W, Lange UE, Seitz W, Höffken HW.
Bioorg Med Chem Lett (2006) 16 : 2641 -2647
PubMed 16517159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.06 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208140 1 8.80
CHEMBL206205 1 8.72
CHEMBL377681 1 8.32
CHEMBL266349 MELAGATRAN 4.0 1 7.92
CHEMBL381709 1 7.68
CHEMBL207981 1 6.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208140 IC50 = 1.6 nM 8.80
CHEMBL206205 IC50 = 1.9 nM 8.72
CHEMBL377681 IC50 = 4.8 nM 8.32
CHEMBL266349 MELAGATRAN IC50 = 11.9 nM 7.92
CHEMBL381709 IC50 = 21.0 nM 7.68
CHEMBL207981 IC50 = 117.0 nM 6.93