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Assay Detail

CHEMBL714218

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Binding
Inhibitory concentration against Matrix metalloprotease-2
14
Total Activities
14
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

Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme.
Holms J, Mast K, Marcotte P, Elmore I, Li J, Pease L, Glaser K, Morgan D, Michaelides M, Davidsen S.
Bioorg Med Chem Lett (2001) 11 : 2907 -2910
PubMed 11677124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.55 10.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318484 1 10.32
CHEMBL99103 1 9.64
CHEMBL318860 1 9.59
CHEMBL98770 1 9.10
CHEMBL318005 1 8.00
CHEMBL99547 1 7.96
CHEMBL99120 1 7.89
CHEMBL99283 1 7.02
CHEMBL95718 1 6.96
CHEMBL98304 1 6.64
CHEMBL99318 1 6.00
CHEMBL329302 1 5.66
CHEMBL329232 1 5.47
CHEMBL316725 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318484 IC50 = 0.048 nM 10.32
CHEMBL99103 IC50 = 0.23 nM 9.64
CHEMBL318860 IC50 = 0.26 nM 9.59
CHEMBL98770 IC50 = 0.79 nM 9.10
CHEMBL318005 IC50 = 10.0 nM 8.00
CHEMBL99547 IC50 = 11.0 nM 7.96
CHEMBL99120 IC50 = 13.0 nM 7.89
CHEMBL99283 IC50 = 96.0 nM 7.02
CHEMBL95718 IC50 = 110.0 nM 6.96
CHEMBL98304 IC50 = 230.0 nM 6.64
CHEMBL99318 IC50 = 1000.0 nM 6.00
CHEMBL329302 IC50 = 2200.0 nM 5.66
CHEMBL329232 IC50 = 3400.0 nM 5.47
CHEMBL316725 IC50 = 4000.0 nM 5.40