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Assay Detail

CHEMBL717495

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Binding
Concentration required to inhibit the catalytic domain Matrix metalloprotease-2 using Nagase fluorogenic as a substrate.
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

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

Publication

Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1).
Fray MJ, Dickinson RP.
Bioorg Med Chem Lett (2001) 11 : 571 -574
PubMed 11229774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.75 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20154 1 9.42
CHEMBL154044 1 9.00
CHEMBL156830 1 7.96
CHEMBL345447 1 7.47
CHEMBL443818 1 7.39
CHEMBL154551 1 7.21
CHEMBL356413 1 7.07
CHEMBL347673 1 7.00
CHEMBL348878 1 6.68
CHEMBL154440 1 6.51
CHEMBL152277 1 6.47
CHEMBL436230 1 6.38
CHEMBL154040 1 6.04
CHEMBL153882 1 5.89
CHEMBL345306 1 5.77
CHEMBL117225 1 5.75
CHEMBL154169 1 5.17
CHEMBL345305 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20154 IC50 = 0.38 nM 9.42
CHEMBL154044 IC50 = 1.0 nM 9.00
CHEMBL156830 IC50 = 11.0 nM 7.96
CHEMBL345447 IC50 = 34.0 nM 7.47
CHEMBL443818 IC50 = 41.0 nM 7.39
CHEMBL154551 IC50 = 61.0 nM 7.21
CHEMBL356413 IC50 = 86.0 nM 7.07
CHEMBL347673 IC50 = 100.0 nM 7.00
CHEMBL348878 IC50 = 210.0 nM 6.68
CHEMBL154440 IC50 = 310.0 nM 6.51
CHEMBL152277 IC50 = 335.0 nM 6.47
CHEMBL436230 IC50 = 414.0 nM 6.38
CHEMBL154040 IC50 = 920.0 nM 6.04
CHEMBL153882 IC50 = 1300.0 nM 5.89
CHEMBL345306 IC50 = 1700.0 nM 5.77
CHEMBL117225 IC50 = 1790.0 nM 5.75
CHEMBL154169 IC50 = 6800.0 nM 5.17
CHEMBL345305 IC50 = 52000.0 nM 4.28