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Assay Detail

CHEMBL815977

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

Binding
In vitro inhibition of HWMT human urokinase Plasminogen activator.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Urokinase-type plasminogen activator (CHEMBL3286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.
Barber CG, Dickinson RP, Horne VA.
Bioorg Med Chem Lett (2002) 12 : 181 -184
PubMed 11755349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 4.83 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293098 1 5.54
CHEMBL54357 1 5.50
CHEMBL55125 1 5.32
CHEMBL292900 1 5.26
CHEMBL41040 1 5.17
CHEMBL54467 1 5.15
CHEMBL55808 1 5.06
CHEMBL298989 1 5.00
CHEMBL128047 1 4.53
CHEMBL53031 1 4.49
CHEMBL52361 1 4.42
CHEMBL53032 1 4.39
CHEMBL55184 1 4.27
CHEMBL300135 1 4.21
CHEMBL54640 1 4.08
CHEMBL54989 1 -
CHEMBL54545 1 -
CHEMBL55051 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293098 Ki = 2900.0 nM 5.54
CHEMBL54357 Ki = 3130.0 nM 5.50
CHEMBL55125 Ki = 4830.0 nM 5.32
CHEMBL292900 Ki = 5470.0 nM 5.26
CHEMBL41040 Ki = 6700.0 nM 5.17
CHEMBL54467 Ki = 7100.0 nM 5.15
CHEMBL55808 Ki = 8700.0 nM 5.06
CHEMBL298989 Ki = 10000.0 nM 5.00
CHEMBL128047 Ki = 29500.0 nM 4.53
CHEMBL53031 Ki = 32300.0 nM 4.49
CHEMBL52361 Ki = 37700.0 nM 4.42
CHEMBL53032 Ki = 40700.0 nM 4.39
CHEMBL55184 Ki = 53300.0 nM 4.27
CHEMBL300135 Ki = 62000.0 nM 4.21
CHEMBL54640 Ki = 83800.0 nM 4.08
CHEMBL54989 Ki = 292000.0 nM -
CHEMBL54545 Ki = 173000.0 nM -
CHEMBL55051 Ki = 147000.0 nM -