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Assay Detail

CHEMBL663502

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

Binding
In vitro inhibitory activity against factor Xa
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.
Huang W, Naughton MA, Yang H, Su T, Dam S, Wong PW, Arfsten A, Edwards S, Sinha U, Hollenbach S, Scarborough RM, Zhu BY.
Bioorg Med Chem Lett (2003) 13 : 723 -728
PubMed 12639567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.80 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL352039 1 9.30
CHEMBL423810 1 9.29
CHEMBL350587 1 9.10
CHEMBL355376 1 8.70
CHEMBL159695 1 8.70
CHEMBL162461 1 8.40
CHEMBL163174 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL352039 IC50 = 0.5 nM 9.30
CHEMBL423810 IC50 = 0.51 nM 9.29
CHEMBL350587 IC50 = 0.79 nM 9.10
CHEMBL355376 IC50 = 2.0 nM 8.70
CHEMBL159695 IC50 = 2.0 nM 8.70
CHEMBL162461 IC50 = 4.0 nM 8.40
CHEMBL163174 IC50 = 8.0 nM 8.10