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Assay Detail

CHEMBL5225194

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

Binding
Inhibition of Heparanase-1 (unknown origin) by HTRF method
13
Total Activities
13
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

Heparanase (CHEMBL3921)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead identification of novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent heparanase-1 inhibitor.
Imai Y, Wakasugi D, Suzuki R, Kato S, Sugisaki M, Mima M, Miyagawa H, Endo M, Fujimoto N, Fukunaga T, Kato S, Kuroda S, Takahashi T, Kakinuma H.
Bioorg Med Chem Lett (2023) 79 : 129050 -129050
PubMed 36368497 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.89 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5273557 1 5.47
CHEMBL5284745 1 5.39
CHEMBL5276305 1 5.10
CHEMBL5280906 1 5.09
CHEMBL3347523 1 5.04
CHEMBL5280810 1 4.95
CHEMBL5290753 1 4.92
CHEMBL5281456 1 4.72
CHEMBL5273519 1 4.71
CHEMBL5279462 1 4.71
CHEMBL5283021 1 4.67
CHEMBL5270267 1 4.52
CHEMBL4650593 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5273557 IC50 = 3410.0 nM 5.47
CHEMBL5284745 IC50 = 4040.0 nM 5.39
CHEMBL5276305 IC50 = 7890.0 nM 5.10
CHEMBL5280906 IC50 = 8030.0 nM 5.09
CHEMBL3347523 IC50 = 9190.0 nM 5.04
CHEMBL5280810 IC50 = 11200.0 nM 4.95
CHEMBL5290753 IC50 = 12000.0 nM 4.92
CHEMBL5281456 IC50 = 19200.0 nM 4.72
CHEMBL5273519 IC50 = 19300.0 nM 4.71
CHEMBL5279462 IC50 = 19700.0 nM 4.71
CHEMBL5283021 IC50 = 21500.0 nM 4.67
CHEMBL5270267 IC50 = 30500.0 nM 4.52
CHEMBL4650593 IC50 = 50100.0 nM 4.30