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Assay Detail

CHEMBL710553

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

Binding
Inhibition of the gelatinase-A enzyme.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

72 kDa type IV collagenase (CHEMBL333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective inhibitors of gelatinase-a 1. hydroxamic acid derivatives
Porter JR, Beeley NR, Boyce BA, Mason B, Millican A, Millar K, Leonard J, Morphy J, O'Connell JP
Bioorg Med Chem Lett (1994) 4 : 2741 -2746
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 9.94 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92453 1 11.00
CHEMBL93583 1 11.00
CHEMBL91655 1 11.00
CHEMBL92828 1 11.00
CHEMBL93395 1 11.00
CHEMBL328092 1 11.00
CHEMBL93791 1 10.70
CHEMBL93235 1 10.70
CHEMBL94114 1 10.70
CHEMBL311397 1 10.52
CHEMBL92600 1 10.52
CHEMBL93695 1 10.52
CHEMBL327472 1 10.30
CHEMBL308511 1 10.22
CHEMBL310037 1 10.22
CHEMBL75403 1 10.21
CHEMBL312076 1 10.10
CHEMBL415074 1 10.00
CHEMBL73803 1 9.60
CHEMBL76519 1 9.52
CHEMBL77754 1 9.48
CHEMBL90743 1 9.23
CHEMBL77808 1 8.65
CHEMBL328005 1 8.16
CHEMBL93890 1 7.48
CHEMBL327780 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92453 Ki = 0.01 nM 11.00
CHEMBL93583 Ki = 0.01 nM 11.00
CHEMBL91655 Ki = 0.01 nM 11.00
CHEMBL92828 Ki = 0.01 nM 11.00
CHEMBL93395 Ki = 0.01 nM 11.00
CHEMBL328092 Ki = 0.01 nM 11.00
CHEMBL93791 Ki = 0.02 nM 10.70
CHEMBL93235 Ki = 0.02 nM 10.70
CHEMBL94114 Ki = 0.02 nM 10.70
CHEMBL311397 Ki = 0.03 nM 10.52
CHEMBL92600 Ki = 0.03 nM 10.52
CHEMBL93695 Ki = 0.03 nM 10.52
CHEMBL327472 Ki = 0.05 nM 10.30
CHEMBL308511 Ki = 0.06 nM 10.22
CHEMBL310037 Ki = 0.06 nM 10.22
CHEMBL75403 Ki = 0.062 nM 10.21
CHEMBL312076 Ki = 0.08 nM 10.10
CHEMBL415074 Ki = 0.1 nM 10.00
CHEMBL73803 Ki = 0.254 nM 9.60
CHEMBL76519 Ki = 0.3 nM 9.52
CHEMBL77754 Ki = 0.33 nM 9.48
CHEMBL90743 Ki = 0.59 nM 9.23
CHEMBL77808 Ki = 2.24 nM 8.65
CHEMBL328005 Ki = 6.9 nM 8.16
CHEMBL93890 Ki = 33.0 nM 7.48
CHEMBL327780 Ki = 1900.0 nM 5.72