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Assay Detail

CHEMBL865716

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

Assay Information

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

Target

Tissue-type plasminogen activator (CHEMBL1873)
Type SINGLE PROTEIN
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 6.65 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208140 1 7.16
CHEMBL206205 1 6.90
CHEMBL381709 1 6.76
CHEMBL377681 1 6.27
CHEMBL207981 1 6.16
CHEMBL266349 MELAGATRAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208140 IC50 = 70.0 nM 7.16
CHEMBL206205 IC50 = 125.0 nM 6.90
CHEMBL381709 IC50 = 173.0 nM 6.76
CHEMBL377681 IC50 = 540.0 nM 6.27
CHEMBL207981 IC50 = 687.0 nM 6.16
CHEMBL266349 MELAGATRAN IC50 - -