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Assay Detail

CHEMBL5040376

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

Binding
Binding affinity to human tissue type plasminogen assessed as inhibition constant using Methanesulfonyl-D-Cyclohexylalanyl-glycylarginine p-Nitroaniline as substrate measured upto 120 mins by spectrophotometric analysis
1
Total Activities
1
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

Tissue-type plasminogen activator (CHEMBL1873)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
Dilger AK, Pabbisetty KB, Corte JR, De Lucca I, Fang T, Yang W, Pinto DJP, Wang Y, Zhu Y, Mathur A, Li J, Hou X, Smith D, Sun D, Zhang H, Krishnananthan S, Wu DR, Myers JE, Sheriff S, Rossi KA, Chacko S, Zheng JJ, Galella MA, Ziemba T, Dierks EA, Bozarth JM, Wu Y, Crain E, Wong PC, Luettgen JM, Wexler RR, Ewing WR.
J Med Chem (2022) 65 : 1770 -1785
PubMed 34494428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.64 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4112929 MILVEXIAN 3.0 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4112929 MILVEXIAN Ki = 2300.0 nM 5.64