Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL714992

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

Binding
In vitro inhibition of Matrix metalloprotease-2
13
Total Activities
13
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 13 5.36 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38851 1 7.50
CHEMBL36615 1 6.40
CHEMBL41892 1 5.23
CHEMBL290067 1 5.10
CHEMBL41923 1 4.72
CHEMBL43026 1 4.46
CHEMBL41067 1 4.12
CHEMBL41928 1 -
CHEMBL289108 1 -
CHEMBL41485 1 -
CHEMBL42862 1 -
CHEMBL39358 1 -
CHEMBL39035 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38851 IC50 = 32.0 nM 7.50
CHEMBL36615 IC50 = 400.0 nM 6.40
CHEMBL41892 IC50 = 5900.0 nM 5.23
CHEMBL290067 IC50 = 8000.0 nM 5.10
CHEMBL41923 IC50 = 19000.0 nM 4.72
CHEMBL43026 IC50 = 35000.0 nM 4.46
CHEMBL41067 IC50 = 76000.0 nM 4.12
CHEMBL41928 IC50 > 100000.0 nM -
CHEMBL289108 IC50 = 650000.0 nM -
CHEMBL41485 IC50 = 260000.0 nM -
CHEMBL42862 IC50 = 950000.0 nM -
CHEMBL39358 IC50 = 160000.0 nM -
CHEMBL39035 IC50 = 480000.0 nM -