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Assay Detail

CHEMBL710982

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Binding
In vitro inhibition of Matrix metalloprotease-2
10
Total Activities
10
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

Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.
Michaelides MR, Dellaria JF, Gong J, Holms JH, Bouska JJ, Stacey J, Wada CK, Heyman HR, Curtin ML, Guo Y, Goodfellow CL, Elmore IB, Albert DH, Magoc TJ, Marcotte PA, Morgan DW, Davidsen SK.
Bioorg Med Chem Lett (2001) 11 : 1553 -1556
PubMed 11412979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.87 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415872 1 5.47
CHEMBL434204 1 5.28
CHEMBL288510 1 5.16
CHEMBL41102 1 5.11
CHEMBL41100 1 5.09
CHEMBL288592 1 4.92
CHEMBL288701 1 4.60
CHEMBL38717 1 4.43
CHEMBL290457 1 4.35
CHEMBL288067 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415872 IC50 = 3400.0 nM 5.47
CHEMBL434204 IC50 = 5200.0 nM 5.28
CHEMBL288510 IC50 = 6900.0 nM 5.16
CHEMBL41102 IC50 = 7800.0 nM 5.11
CHEMBL41100 IC50 = 8200.0 nM 5.09
CHEMBL288592 IC50 = 12000.0 nM 4.92
CHEMBL288701 IC50 = 25000.0 nM 4.60
CHEMBL38717 IC50 = 37000.0 nM 4.43
CHEMBL290457 IC50 = 45000.0 nM 4.35
CHEMBL288067 IC50 = 58000.0 nM 4.24