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Assay Detail

CHEMBL1942016

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

Binding
Inhibition of MMP1 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 4 hrs measured every 15 secs for 20 mins by fluorescence analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases.
Marques SM, Tuccinardi T, Nuti E, Santamaria S, André V, Rossello A, Martinelli A, Santos MA.
J Med Chem (2011) 54 : 8289 -8298
PubMed 22017477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.67 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1939845 1 5.89
CHEMBL1939846 1 5.80
CHEMBL1939844 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1939845 IC50 = 1300.0 nM 5.89
CHEMBL1939846 IC50 = 1600.0 nM 5.80
CHEMBL1939844 IC50 = 4900.0 nM 5.31