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Assay Detail

CHEMBL4618308

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

Binding
Inhibition of human tissue-type plasminogen activator using methyl-sulfonyl-D-cyclohexylalanyl-Gly-Arg-pNA substrate by spectrophotometry
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 a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.
Yang W, Wang Y, Lai A, Clark CG, Corte JR, Fang T, Gilligan PJ, Jeon Y, Pabbisetty KB, Rampulla RA, Mathur A, Kaspady M, Neithnadka PR, Arumugam A, Raju S, Rossi KA, Myers JE, Sheriff S, Lou Z, Zheng JJ, Chacko SA, Bozarth JM, Wu Y, Crain EJ, Wong PC, Seiffert DA, Luettgen JM, Lam PYS, Wexler RR, Ewing WR.
J Med Chem (2020) 63 : 7226 -7242
PubMed 32456431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.39 5.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4638245 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4638245 Ki = 4100.0 nM 5.39