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Assay Detail

CHEMBL1042363

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

Binding
Inhibition of autoactivated human pro-MMP12 after 1 hr preincubation by fluorimetry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Macrophage metalloelastase (CHEMBL4393)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Nuti E, Panelli L, Casalini F, Avramova SI, Orlandini E, Santamaria S, Nencetti S, Tuccinardi T, Martinelli A, Cercignani G, D'Amelio N, Maiocchi A, Uggeri F, Rossello A.
J Med Chem (2009) 52 : 6347 -6361
PubMed 19775099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.95 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573715 1 9.07
CHEMBL573936 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573715 IC50 = 0.85 nM 9.07
CHEMBL573936 IC50 = 150.0 nM 6.82