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Assay Detail

CHEMBL715840

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Binding
Inhibition of human Matrix metalloprotease-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

Heterocycle-based MMP inhibitors with P2' substituents.
Pikul S, Dunham KM, Almstead NG, De B, Natchus MG, Taiwo YO, Williams LE, Hynd BA, Hsieh LC, Janusz MJ, Gu F, Mieling GE.
Bioorg Med Chem Lett (2001) 11 : 1009 -1013
PubMed 11327577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.67 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427616 1 9.30
CHEMBL415482 1 9.17
CHEMBL269019 1 9.15
CHEMBL7108 1 9.00
CHEMBL7390 1 9.00
CHEMBL267939 1 8.80
CHEMBL7756 1 8.62
CHEMBL268114 1 8.57
CHEMBL266292 1 8.47
CHEMBL6572 1 8.28
CHEMBL268377 1 8.28
CHEMBL6973 1 8.06
CHEMBL514138 CGS-27023A 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427616 IC50 = 0.5 nM 9.30
CHEMBL415482 IC50 = 0.68 nM 9.17
CHEMBL269019 IC50 = 0.7 nM 9.15
CHEMBL7108 IC50 = 1.0 nM 9.00
CHEMBL7390 IC50 = 1.0 nM 9.00
CHEMBL267939 IC50 = 1.6 nM 8.80
CHEMBL7756 IC50 = 2.4 nM 8.62
CHEMBL268114 IC50 = 2.7 nM 8.57
CHEMBL266292 IC50 = 3.4 nM 8.47
CHEMBL6572 IC50 = 5.2 nM 8.28
CHEMBL268377 IC50 = 5.3 nM 8.28
CHEMBL6973 IC50 = 8.8 nM 8.06
CHEMBL514138 CGS-27023A IC50 = 9.1 nM 8.04