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Assay Detail

CHEMBL902751

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

Binding
Inhibition of human thrombin
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Prothrombin (CHEMBL204)
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 15 5.47 6.54
Ki 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL238707 1 6.54
CHEMBL391968 1 6.41
CHEMBL214814 1 6.11
CHEMBL239331 1 6.11
CHEMBL393979 1 5.95
CHEMBL239118 1 5.63
CHEMBL239535 1 5.62
CHEMBL239536 1 5.42
CHEMBL391344 1 5.09
CHEMBL238491 1 4.92
CHEMBL238913 1 4.77
CHEMBL393591 1 4.77
CHEMBL238708 1 4.70
CHEMBL239747 1 4.49
CHEMBL391969 1 -
CHEMBL238493 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL238707 IC50 = 288.0 nM 6.54
CHEMBL391968 IC50 = 390.0 nM 6.41
CHEMBL214814 IC50 = 770.0 nM 6.11
CHEMBL239331 IC50 = 780.0 nM 6.11
CHEMBL393979 IC50 = 1130.0 nM 5.95
CHEMBL239118 IC50 = 2350.0 nM 5.63
CHEMBL239535 IC50 = 2400.0 nM 5.62
CHEMBL239536 IC50 = 3800.0 nM 5.42
CHEMBL391344 IC50 = 8100.0 nM 5.09
CHEMBL238491 IC50 = 11900.0 nM 4.92
CHEMBL238913 IC50 = 17000.0 nM 4.77
CHEMBL393591 IC50 = 17000.0 nM 4.77
CHEMBL238708 IC50 = 20000.0 nM 4.70
CHEMBL239747 IC50 = 32200.0 nM 4.49
CHEMBL391969 Ki > 1000000.0 nM -
CHEMBL238493 IC50 = 125000.0 nM -