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Assay Detail

CHEMBL710596

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

Binding
In vitro inhibitory activity against matrix metalloprotease 1 isolated from the culture medium of human skin fibroblasts induced with PMA
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Sheppard GS, Florjancic AS, Giesler JR, Xu L, Guo Y, Davidsen SK, Marcotte PA, Elmore I, Albert DH, Magoc TJ, Bouska JJ, Goodfellow CL, Morgan DW, Summers JB.
Bioorg Med Chem Lett (1998) 8 : 3251 -3256
PubMed 9873712 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 8.27 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321180 1 9.59
CHEMBL432991 1 8.96
CHEMBL279785 MARIMASTAT 3.0 1 8.96
CHEMBL279786 BATIMASTAT 2.0 1 8.92
CHEMBL111798 1 8.92
CHEMBL418292 1 8.74
CHEMBL320045 1 8.72
CHEMBL62007 1 8.68
CHEMBL432079 1 8.66
CHEMBL324664 1 8.59
CHEMBL430524 1 8.57
CHEMBL110696 1 8.33
CHEMBL324874 1 8.32
CHEMBL432397 1 8.30
CHEMBL325940 1 8.30
CHEMBL320782 1 8.29
CHEMBL411851 1 8.21
CHEMBL111736 1 8.04
CHEMBL111104 1 8.00
CHEMBL325552 1 7.89
CHEMBL109596 1 7.85
CHEMBL109706 1 7.40
CHEMBL109239 1 7.22
CHEMBL109246 1 6.75
CHEMBL321602 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321180 IC50 = 0.26 nM 9.59
CHEMBL432991 IC50 = 1.1 nM 8.96
CHEMBL279785 MARIMASTAT IC50 = 1.1 nM 8.96
CHEMBL279786 BATIMASTAT IC50 = 1.2 nM 8.92
CHEMBL111798 IC50 = 1.2 nM 8.92
CHEMBL418292 IC50 = 1.8 nM 8.74
CHEMBL320045 IC50 = 1.9 nM 8.72
CHEMBL62007 IC50 = 2.1 nM 8.68
CHEMBL432079 IC50 = 2.2 nM 8.66
CHEMBL324664 IC50 = 2.6 nM 8.59
CHEMBL430524 IC50 = 2.7 nM 8.57
CHEMBL110696 IC50 = 4.7 nM 8.33
CHEMBL324874 IC50 = 4.8 nM 8.32
CHEMBL432397 IC50 = 5.0 nM 8.30
CHEMBL325940 IC50 = 5.0 nM 8.30
CHEMBL320782 IC50 = 5.1 nM 8.29
CHEMBL411851 IC50 = 6.2 nM 8.21
CHEMBL111736 IC50 = 9.1 nM 8.04
CHEMBL111104 IC50 = 10.0 nM 8.00
CHEMBL325552 IC50 = 13.0 nM 7.89
CHEMBL109596 IC50 = 14.0 nM 7.85
CHEMBL109706 IC50 = 40.0 nM 7.40
CHEMBL109239 IC50 = 60.0 nM 7.22
CHEMBL109246 IC50 = 180.0 nM 6.75
CHEMBL321602 IC50 = 270.0 nM 6.57