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Assay Detail

CHEMBL4374437

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

Binding
Inhibition of recombinant factor Xa (unknown origin) using Bz-Ile-Glu-Gly-Arg-pNA as substrate preincubated for 30 mins followed by substrate addition by chromogenic assay
18
Total Activities
18
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

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

Publication

Piperidine carbamate peptidomimetic inhibitors of the serine proteases HGFA, matriptase and hepsin.
Damalanka VC, Wildman SA, Janetka JW.
Medchemcomm (2019) 10 : 1646 -1655
PubMed 31803403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.73 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454016 1 6.58
CHEMBL3781349 1 6.42
CHEMBL4530678 1 5.70
CHEMBL4540950 1 5.42
CHEMBL4469962 1 5.19
CHEMBL4527923 1 5.05
CHEMBL4452723 1 -
CHEMBL4559504 1 -
CHEMBL4448976 1 -
CHEMBL4472744 1 -
CHEMBL4558850 1 -
CHEMBL4541290 1 -
CHEMBL4453382 1 -
CHEMBL4537657 1 -
CHEMBL4469506 1 -
CHEMBL4436751 1 -
CHEMBL4434900 1 -
CHEMBL4462597 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454016 IC50 = 260.0 nM 6.58
CHEMBL3781349 IC50 = 380.0 nM 6.42
CHEMBL4530678 IC50 = 2000.0 nM 5.70
CHEMBL4540950 IC50 = 3800.0 nM 5.42
CHEMBL4469962 IC50 = 6500.0 nM 5.19
CHEMBL4527923 IC50 = 9000.0 nM 5.05
CHEMBL4452723 IC50 > 20000.0 nM -
CHEMBL4559504 IC50 - -
CHEMBL4448976 IC50 - -
CHEMBL4472744 IC50 - -
CHEMBL4558850 IC50 - -
CHEMBL4541290 IC50 - -
CHEMBL4453382 IC50 > 20000.0 nM -
CHEMBL4537657 IC50 - -
CHEMBL4469506 IC50 - -
CHEMBL4436751 IC50 - -
CHEMBL4434900 IC50 - -
CHEMBL4462597 IC50 > 20000.0 nM -