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Assay Detail

CHEMBL4676491

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

Binding
Inhibition of human uPA using Tos-Gly-Pro-Arg-AMC as fluorogenic substrate measured at 1 min interval for 1 hr by fluorometric assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Urokinase-type plasminogen activator (CHEMBL3286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acylated 1H-1,2,4-Triazol-5-amines Targeting Human Coagulation Factor XIIa and Thrombin: Conventional and Microscale Synthesis, Anticoagulant Properties, and Mechanism of Action.
Korff M,Imberg L,Will JM,Bückreiß N,Kalinina SA,Wenzel BM,Kastner GA,Daniliuc CG,Barth M,Ovsepyan RA,Butov KR,Humpf HU,Lehr M,Panteleev MA,Poso A,Karst U,Steinmetzer T,Bendas G,Kalinin DV
J Med Chem (2020) 63 : 13159 -13186
PubMed 33089691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.27 5.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4777212 1 5.53
CHEMBL4754247 1 5.17
CHEMBL4748137 1 5.10
CHEMBL4776259 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4777212 IC50 = 2942.0 nM 5.53
CHEMBL4754247 IC50 = 6762.0 nM 5.17
CHEMBL4748137 IC50 = 7930.0 nM 5.10
CHEMBL4776259 IC50 > 5000.0 nM -