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Assay Detail

CHEMBL716607

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

Binding
Inhibition of Matrix metalloprotease-2 (MMP-2)
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 Expert

Target

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

Publication

Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.
Curtin ML, Garland RB, Davidsen SK, Marcotte PA, Albert DH, Magoc TJ, Hutchins C.
Bioorg Med Chem Lett (1998) 8 : 1443 -1448
PubMed 9873367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.88 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32730 1 8.89
CHEMBL432079 1 8.74
CHEMBL32839 1 8.64
CHEMBL33306 1 8.60
CHEMBL35348 1 8.38
CHEMBL32285 1 8.21
CHEMBL286788 1 7.64
CHEMBL35602 1 7.46
CHEMBL286295 1 7.30
CHEMBL33418 1 7.28
CHEMBL286698 1 7.19
CHEMBL289003 1 7.18
CHEMBL284465 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32730 IC50 = 1.3 nM 8.89
CHEMBL432079 IC50 = 1.8 nM 8.74
CHEMBL32839 IC50 = 2.3 nM 8.64
CHEMBL33306 IC50 = 2.5 nM 8.60
CHEMBL35348 IC50 = 4.2 nM 8.38
CHEMBL32285 IC50 = 6.2 nM 8.21
CHEMBL286788 IC50 = 23.0 nM 7.64
CHEMBL35602 IC50 = 35.0 nM 7.46
CHEMBL286295 IC50 = 50.0 nM 7.30
CHEMBL33418 IC50 = 52.0 nM 7.28
CHEMBL286698 IC50 = 64.0 nM 7.19
CHEMBL289003 IC50 = 66.0 nM 7.18
CHEMBL284465 IC50 = 110.0 nM 6.96