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Assay Detail

CHEMBL941546

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

Binding
Inhibition of human MMP2 by fluorescence assay
20
Total Activities
20
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

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

Publication

Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.
Bailey S, Fish PV, Billotte S, Bordner J, Greiling D, James K, McElroy A, Mills JE, Reed C, Webster R.
Bioorg Med Chem Lett (2008) 18 : 6562 -6567
PubMed 18945617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.92 6.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL154551 1 6.87
CHEMBL154040 1 6.00
CHEMBL229375 1 5.23
CHEMBL481712 1 4.66
CHEMBL482341 1 4.30
CHEMBL480351 1 4.13
CHEMBL374840 1 4.10
CHEMBL482319 1 4.09
CHEMBL226686 1 -
CHEMBL480757 1 -
CHEMBL480191 1 -
CHEMBL481711 1 -
CHEMBL520087 1 -
CHEMBL518467 1 -
CHEMBL226630 1 -
CHEMBL521410 1 -
CHEMBL480758 1 -
CHEMBL480192 1 -
CHEMBL525215 1 -
CHEMBL521443 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL154551 IC50 = 135.0 nM 6.87
CHEMBL154040 IC50 = 1000.0 nM 6.00
CHEMBL229375 IC50 = 5900.0 nM 5.23
CHEMBL481712 IC50 = 21700.0 nM 4.66
CHEMBL482341 IC50 = 50500.0 nM 4.30
CHEMBL480351 IC50 = 74900.0 nM 4.13
CHEMBL374840 IC50 = 80000.0 nM 4.10
CHEMBL482319 IC50 = 81800.0 nM 4.09
CHEMBL226686 IC50 > 100000.0 nM -
CHEMBL480757 IC50 > 100000.0 nM -
CHEMBL480191 IC50 > 100000.0 nM -
CHEMBL481711 IC50 > 30000.0 nM -
CHEMBL520087 IC50 > 30000.0 nM -
CHEMBL518467 IC50 > 30000.0 nM -
CHEMBL226630 IC50 > 60000.0 nM -
CHEMBL521410 IC50 - -
CHEMBL480758 IC50 - -
CHEMBL480192 IC50 - -
CHEMBL525215 IC50 - -
CHEMBL521443 IC50 - -