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Assay Detail

CHEMBL902753

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Binding
Inhibition of factor 10a
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.
Joossens J, Ali OM, El-Sayed I, Surpateanu G, Van der Veken P, Lambeir AM, Setyono-Han B, Foekens JA, Schneider A, Schmalix W, Haemers A, Augustyns K.
J Med Chem (2007) 50 : 6638 -6646
PubMed 18052026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.54 5.22
Ki 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL238707 1 5.22
CHEMBL238913 1 4.86
CHEMBL391916 1 4.70
CHEMBL391344 1 4.57
CHEMBL393979 1 4.52
CHEMBL214814 1 4.47
CHEMBL391968 1 4.00
CHEMBL239535 1 4.00
CHEMBL391969 1 -
CHEMBL238493 1 -
CHEMBL393592 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL238707 IC50 = 6000.0 nM 5.22
CHEMBL238913 IC50 = 13700.0 nM 4.86
CHEMBL391916 IC50 = 20000.0 nM 4.70
CHEMBL391344 IC50 = 27000.0 nM 4.57
CHEMBL393979 IC50 = 30000.0 nM 4.52
CHEMBL214814 IC50 = 33500.0 nM 4.47
CHEMBL391968 IC50 = 100000.0 nM 4.00
CHEMBL239535 IC50 = 100000.0 nM 4.00
CHEMBL391969 Ki > 1000000.0 nM -
CHEMBL238493 IC50 = 250000.0 nM -
CHEMBL393592 IC50 > 250000.0 nM -