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Assay Detail

CHEMBL5127308

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

Binding
Inhibition of thrombin in human blood using fluorogenic Ac-FVR-AMC as substrate by chromogenic assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs.
Li X, Guo T, Feng Q, Bai T, Wu L, Liu Y, Zheng X, Jia J, Pei J, Wu S, Song Y, Zhang Y.
Eur J Med Chem (2022) 228 : 114035 -114035
PubMed 34902735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.31 8.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48361 DABIGATRAN 3.0 1 8.58
CHEMBL3415215 1 8.47
CHEMBL3415211 1 8.31
CHEMBL3415064 1 8.25
CHEMBL3415065 1 8.14
CHEMBL3415210 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48361 DABIGATRAN IC50 = 2.61 nM 8.58
CHEMBL3415215 IC50 = 3.39 nM 8.47
CHEMBL3415211 IC50 = 4.92 nM 8.31
CHEMBL3415064 IC50 = 5.63 nM 8.25
CHEMBL3415065 IC50 = 7.26 nM 8.14
CHEMBL3415210 IC50 = 8.4 nM 8.08