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Assay Detail

CHEMBL860314

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

Binding
Inhibitory activity against human platelet heparanase by Microcon ultrafiltration assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Heparanase (CHEMBL3921)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological activity, and preliminary pharmacokinetic evaluation of analogues of a phosphosulfomannan angiogenesis inhibitor (PI-88).
Karoli T, Liu L, Fairweather JK, Hammond E, Li CP, Cochran S, Bergefall K, Trybala E, Addison RS, Ferro V.
J Med Chem (2005) 48 : 8229 -8236
PubMed 16366604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.74 5.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198643 1 5.79
CHEMBL382044 1 5.74
CHEMBL262707 1 5.73
CHEMBL265885 1 5.70
CHEMBL373279 1 -
CHEMBL264593 1 -
CHEMBL438743 1 -
CHEMBL412087 1 -
CHEMBL405383 1 -
CHEMBL264125 1 -
CHEMBL413401 1 -
CHEMBL425275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198643 IC50 = 1640.0 nM 5.79
CHEMBL382044 IC50 = 1830.0 nM 5.74
CHEMBL262707 IC50 = 1850.0 nM 5.73
CHEMBL265885 IC50 = 2020.0 nM 5.70
CHEMBL373279 IC50 - -
CHEMBL264593 IC50 - -
CHEMBL438743 IC50 - -
CHEMBL412087 IC50 - -
CHEMBL405383 IC50 - -
CHEMBL264125 IC50 - -
CHEMBL413401 IC50 - -
CHEMBL425275 IC50 - -